QuickLinks -- Click here to rapidly navigate through this document

As filed with the Securities and Exchange Commission on October 9, 2007.

Registration No. 333-145844



UNITED STATES
SECURITIES AND EXCHANGE COMMISSION
WASHINGTON, D.C. 20549


Amendment No. 1
to
FORM S-1
REGISTRATION STATEMENT
UNDER
THE SECURITIES ACT OF 1933


ANACOR PHARMACEUTICALS, INC.
(Exact name of registrant as specified in its charter)

Delaware
(State or other jurisdiction of
incorporation or organization)
  2834
(Primary Standard Industrial
Classification Code Number)
  25-1854385
(I.R.S. Employer
Identification No.)

1060 East Meadow Circle
Palo Alto, CA 94303-4230
(650) 739-0700

(Address, including zip code, and telephone number, including
area code, of registrant's principal executive offices)

David P. Perry
President and Chief Executive Officer
Anacor Pharmaceuticals, Inc.
1060 East Meadow Circle
Palo Alto, CA 94303-4230
(650) 739-0700
(Name, address, including zip code, and telephone number, including area code, of agent for service)




Copies to:
Mark B. Weeks
Stephen B. Thau
Heller Ehrman LLP
275 Middlefield Road
Menlo Park, CA 94025
Telephone: (650) 324-7000
Facsimile: (650) 324-0638
  Bruce K. Dallas
Martin A. Wellington
Davis Polk & Wardwell
1600 El Camino Real
Menlo Park, California 94025
Telephone: (650) 752-2000

         Approximate date of commencement of proposed sale to the public: As soon as practicable after this registration statement becomes effective.


        If any of the securities being registered on this Form are to be offered on a delayed or continuous basis pursuant to Rule 415 under the Securities Act of 1933, check the following box.     o

        If this Form is filed to register additional securities for an offering pursuant to Rule 462(b) under the Securities Act, check the following box and list the Securities Act registration statement number of the earlier effective registration statement for the same offering.     o

        If this Form is a post-effective amendment filed pursuant to Rule 462(c) under the Securities Act, check the following box and list the Securities Act registration statement number of the earlier effective registration statement for the same offering.     o

        If this Form is a post-effective amendment filed pursuant to Rule 462(d) under the Securities Act, check the following box and list the Securities Act registration statement number of the earlier effective registration statement for the same offering.     o


         The registrant hereby amends this registration statement on such date or dates as may be necessary to delay its effective date until the registrant shall file a further amendment which specifically states that this registration statement shall thereafter become effective in accordance with Section 8(a) of the Securities Act of 1933 or until this registration statement shall become effective on such date as the Securities and Exchange Commission, acting pursuant to said Section 8(a), may determine.




PROSPECTUS (Subject to Completion)
Issued October 9, 2007

The information in this prospectus is not complete and may be changed. We may not sell these securities until the registration statement filed with the Securities and Exchange Commission is effective. This prospectus is not an offer to sell these securities and we are not soliciting offers to buy these securities in any state where the offer or sale is not permitted.

                              Shares

LOGO

COMMON STOCK


Anacor Pharmaceuticals, Inc. is offering                              shares of its common stock. This is our initial public offering and no public market currently exists for our shares. We anticipate that the initial public offering price will be between $                and $                per share.


We have applied to have our common stock approved for listing on the Nasdaq Global Market under the symbol "ANAC."


Concurrent with this offering, Schering-Plough and GSK have each agreed to purchase in private placements $10 million in common stock at the initial public offering price. A portion of the stock being sold to Schering-Plough will be purchased from certain of our stockholders.


Investing in our common stock involves risks. See "Risk Factors" beginning on page 9.


PRICE $           A SHARE


 
  Price to
Public

  Underwriting
Discounts and
Commissions

  Proceeds to
Company

Per Share   $   $   $
Total   $                      $                      $                   

We have granted the underwriters the right to purchase up to an additional                            shares of common stock to cover over-allotments.

The Securities and Exchange Commission and state securities regulators have not approved or disapproved these securities, or determined if this prospectus is truthful or complete.    Any representation to the contrary is a criminal offense.

Morgan Stanley & Co. Incorporated expects to deliver the shares to purchasers on                        , 2007.


MORGAN STANLEY   COWEN AND COMPANY

   

                      PACIFIC GROWTH EQUITIES, LLC  

 

NEEDHAM & COMPANY, LLC

 

                        , 2007



TABLE OF CONTENTS

 
  Page
Prospectus Summary   2
Risk Factors   9
Special Note Regarding Forward-Looking Statements   34
Use of Proceeds   35
Dividend Policy   36
Capitalization   37
Dilution   39
Selected Financial Data   41
Management's Discussion and Analysis of Financial Condition and Results of Operations   43
Business   57
Management   80
Compensation Discussion and Analysis   88
Certain Relationships and Related Party Transactions   106
Principal Stockholders   110
Description of Capital Stock   113
Shares Eligible For Future Sale   118
Material United States Federal Income and Estate Tax Consequences to Non-U.S. Holders   120
Underwriters   123
Legal Matters   127
Experts   127
Where You Can Find Additional Information   127
Index To Financial Statements   F-1

        You should rely only on the information contained in this prospectus or in any free writing prospectus we may authorize to be delivered to you. We have not authorized anyone to provide you with information different from that contained in this prospectus. We are offering to sell, and seeking offers to buy, shares of common stock only in jurisdictions where offers and sales are permitted. The information contained in this prospectus is accurate only as of the date on the front cover of this prospectus, or other date stated in this prospectus, regardless of the time of delivery of this prospectus or of any sale of our common stock.

         Until                       , 2007 (25 days after commencement of this offering), all dealers that buy, sell, or trade shares of our common stock, whether or not participating in this offering, may be required to deliver a prospectus. This delivery requirement is in addition to the obligation of dealers to deliver a prospectus when acting as underwriters and with respect to their unsold allotments or subscriptions.

        For investors outside the United States: Neither we nor any of the underwriters have done anything that would permit this offering or possession or distribution of this prospectus in any jurisdiction where action for that purpose is required, other than in the United States. You are required to inform yourselves about and to observe any restrictions relating to this offering and the distribution of this prospectus.



PROSPECTUS SUMMARY

         This summary highlights information contained elsewhere in this prospectus and does not contain all of the information you should consider in making your investment decision. You should read this summary together with the more detailed information, including our financial statements and the related notes, elsewhere in this prospectus. You should carefully consider, among other things, the matters discussed in "Risk Factors."


ANACOR PHARMACEUTICALS, INC.

Corporate Overview

        We are a biopharmaceutical company developing novel small-molecule therapeutics derived from our boron chemistry platform. We believe that our expertise in creating new boron-based compounds enables us to develop proprietary product candidates rapidly and cost-effectively that address unmet medical needs across many therapeutic areas. We have focused initially on developing topical applications of our compounds to treat fungal, bacterial and inflammatory diseases. We believe topical therapeutics generally have lower development costs, reduced risk of side effects and faster time to market than systemic therapeutics.

        Our most advanced product candidate is AN2690, a novel topical antifungal in development for the treatment of toenail onychomycosis, a fungal infection of the nail and nail bed. In February 2007, we entered into a worldwide license, development and commercialization agreement with Schering Corporation, or Schering-Plough, for AN2690 for all indications including the treatment of onychomycosis. Pending discussions with the FDA and the outcome of certain non-clinical testing of AN2690, we currently anticipate that Schering-Plough will initiate Phase 3 clinical trials for AN2690 in onychomycosis by the end of 2008. We also have a portfolio of other topical product candidates in development for the treatment of psoriasis, gingivitis, acne, vaginal candidiasis and tinea pedis. All of our product candidates are presently in clinical trials or earlier stages of development and none has received FDA or other regulatory approval for commercial sale. To date, we have not generated any revenue from the sale of our products.

        In October 2007, we entered into a research and development collaboration, option and license agreement with SmithKline Beecham d/b/a GlaxoSmithKline, or GSK, for the discovery, development, manufacture and worldwide commercialization of novel systemic therapeutics for viral and bacterial diseases utilizing our boron-based chemistry. We will be primarily responsible for the discovery and development of each product candidate from the research stage until GSK exercises an option to obtain an exclusive license to such product candidate, at which point GSK will assume sole responsibility for the further development and commercialization of such product candidate on a worldwide basis.

        Our core technology platform is based on the use of boron to develop novel product candidates, which we believe confers a number of advantages in our drug development efforts. Boron-based compounds interact with biological targets in novel ways, and can address targets not amenable to intervention by traditional, carbon-based compounds. We have demonstrated that our boron-based compounds have antibiotic, anti-inflammatory, antiparasitic and antifungal properties, giving them broad utility across multiple disease areas. Technological advances in the synthesis of boron-based compounds have allowed us to rapidly create large families of compounds with drug-like properties. Finally, we believe the intellectual property landscape for boron-based pharmaceutical products is relatively unencumbered compared to that for carbon-based products, providing an attractive opportunity for us to build our intellectual property portfolio.

        By exploiting these advantages of our boron chemistry platform, we have discovered and advanced into clinical development several novel and proprietary boron-based product candidates that address attractive market opportunities.

2



Our Product Candidates

        Our objective is to discover, develop and commercialize proprietary boron-based drug compounds with superior efficacy, safety and convenience for the treatment of a variety of diseases. Our current proprietary product candidates include the following:

3


Our Development and Commercialization Strategy

        We believe topical therapeutics generally have lower development costs, reduced risks of side effects and a faster time to market than systemic products. We intend to develop our topical compounds ourselves through proof of concept studies, which are designed to demonstrate initial indications of safety and effectiveness, or pivotal trials, which are designed to confirm their safety and effectiveness for a particular indication in a larger population to support regulatory approval. Initially, we intend to partner programs for potential systemic compounds at an early stage of development, as demonstrated by our agreement with GSK. We expect that under such alliances, we will undertake early research and initial clinical development of resulting product candidates. We intend to commercialize our products in specialty markets in the United States and to seek commercialization partners for international markets and non-specialty U.S. markets.

Our Agreement with Schering-Plough

        In February 2007, we entered into an exclusive license, development and commercialization agreement with Schering-Plough for the development and worldwide commercialization of AN2690, including for the treatment of onychomycosis. Pursuant to the agreement, Schering-Plough paid us a $40 million up-front fee and we have the right to require Schering-Plough to purchase up to $10 million of our capital stock. In addition to assuming sole responsibility for the costs of development and commercialization of AN2690, Schering-Plough has also agreed to pay us double-digit royalties up to twenty percent on sales of AN2690 and up to an additional $505 million if certain development, regulatory and commercial milestones for onychomycosis are achieved. Schering-Plough is also obligated to pay us additional fees for each additional indication for which Schering-Plough develops AN2690 treatments if certain milestones are achieved. We retained the option to co-promote AN2690 for the treatment of onychomycosis to dermatologists in the United States, subject to certain conditions. Schering-Plough did not acquire any rights to any of our other product candidates under this agreement.

Our Agreement with GSK

        In October 2007, we entered into a research and development collaboration, option and license agreement with GSK for the discovery, development, manufacture and worldwide commercialization of boron-based systemic therapeutics for at least eight product options in up to four target-based projects, one of which will target the Hepatitis C Virus (HCV) and others of which will be in the area of antibiotics. Under the agreement, we will collaborate with GSK to identify and develop boron-based small molecule product candidates.

        Pursuant to the agreement, GSK is obligated to pay us a $12 million up-front fee in October 2007 and we have the right to require GSK to purchase $10 million of our capital stock. In each project, GSK has the option to obtain an exclusive license to develop, commercialize and market worldwide a specified number of product candidates once they have achieved proof of concept criteria. In the HCV project, GSK also has an option to obtain an exclusive license at the time a product candidate is selected. We will be primarily responsible for the discovery and development of each product candidate from the research stage until GSK exercises an option for such product candidate, at which point GSK will assume sole responsibility for the further development and commercialization of such product candidate. GSK is obligated to make payments to us if certain milestones are met, which range up to $252 million to $331 million in the aggregate per product candidate. GSK is further obligated to pay us double-digit tiered royalties based on sales achieved on optioned compounds. In the event that GSK exercises its option for a product candidate

4



in the HCV project at the candidate selection stage, milestone payments for which we are eligible and the product royalties payable to us would be lower.

Risk Related to Our Business

        In executing our business strategy, we face significant risks and uncertainties, as more fully described in the section entitled "Risk Factors." For example:

Concurrent Private Placements

        Concurrent with this offering, Schering-Plough and GSK have agreed to purchase directly from us in private placements $       million and $10 million, respectively, in shares of our common stock at the initial public offering price. In addition, concurrent with this offering, Schering-Plough has agreed to purchase from certain of our stockholders in a private placement $         million in shares of our common stock at the initial public offering price.

Corporate Information

        We were incorporated in Delaware in December 2000 as AnaMax, Inc. We began operations in March 2002 and changed our name to Anacor Pharmaceuticals, Inc. in October 2002. Our principal executive offices are located at 1060 East Meadow Circle, Palo Alto, CA 94303-4230, and our telephone number is (650) 739-0700. Our website address is www.anacor.com . The information on, or accessible through, our website is not part of this prospectus.

        Anacor™ and Anacor Pharmaceuticals™ are our trademarks. This prospectus also contains trademarks and trade names of other companies.

5



THE OFFERING

Common stock offered by us               shares

Common stock sold to GSK in the concurrent private placement

 

            shares

Common stock sold to Schering-Plough by us in the concurrent private placement

 

            shares

Over-allotment option

 

            shares

Common stock to be outstanding after this offering

 

            shares

Use of proceeds

 

We plan to use the proceeds of this offering and the funds we receive from the concurrent private placements to Schering-Plough and GSK to fund our research and development activities, including preclinical studies and clinical trials for our development programs, to increase our working capital and to provide funding for general corporate purposes. See "Use of Proceeds."

Proposed NASDAQ Global Market symbol

 

ANAC

        The number of shares of common stock to be outstanding immediately after this offering is based on 47,627,080 shares of common stock outstanding as of June 30, 2007 and excludes:

Except as otherwise indicated, all information in this prospectus assumes:

Share numbers in this prospectus do not reflect a reverse stock split that we expect to effect prior to completion of this offering.

6



SUMMARY FINANCIAL DATA

        The following summary financial data should be read together with our financial statements and accompanying notes and "Management's Discussion and Analysis of Financial Condition and Results of Operations" appearing elsewhere in this prospectus. The summary financial data in this section is not intended to replace our financial statements and the accompanying notes. Our historical results are not necessarily indicative of our future results.

        We derived the statements of operations data for 2004, 2005 and 2006 from our audited financial statements appearing elsewhere in this prospectus. The statements of operations data for the six months ended June 30, 2006 and 2007 and the balance sheet data as of June 30, 2007 is derived from our unaudited condensed financial statements appearing elsewhere in this prospectus.

 
  Year Ended December 31,
  Six Months Ended
June 30,

 
 
  2004
  2005
  2006
  2006
  2007
 
 
   
   
   
  (unaudited)

 
 
  (in thousands, except share and per share data)

 
Statement of Operations Data:                                
Revenues   $ 7,052   $ 107   $ 861   $ 308   $ 9,320  
Operating expenses                                
  Research and development     10,586     14,023     16,627     7,754     10,164  
  General and administrative     1,646     2,827     3,629     1,656     4,143  
   
 
 
 
 
 
      Total operating expenses     12,232     16,850     20,256     9,410     14,307  
   
 
 
 
 
 
Loss from operations     (5,180 )   (16,743 )   (19,395 )   (9,102 )   (4,987 )
  Interest income     31     343     311     138     571  
  Interest and other expenses, net     (42 )   (44 )   (505 )       (950 )
   
 
 
 
 
 
Net loss   $ (5,191 ) $ (16,444 ) $ (19,589 ) $ (8,964 ) $ (5,366 )
   
 
 
 
 
 
Net loss per share-basic and diluted (1)   $ (1.10 ) $ (3.18 ) $ (3.17 ) $ (1.52 ) $ (0.79 )
   
 
 
 
 
 
Weighted average shares outstanding used in calculating net loss per share-basic and diluted (1)     4,713,871     5,173,237     6,172,694     5,878,624     6,757,945  
   
 
 
 
 
 
Pro forma net loss per share-basic and diluted (1)               $ (0.43 )       $ (0.11 )
               
       
 
Pro forma weighted average shares outstanding used in calculating net loss per share-basic and diluted (1)                 45,706,365           47,600,305  
               
       
 

(1)
Please see Note 2 to our financial statements appearing elsewhere in this prospectus for an explanation of the method used to calculate basic and diluted net loss per common share, the pro forma basic and diluted net loss per common share and the number of shares used in the computation of the per share amounts.

7


 
  As of June 30, 2007
 
  Actual
  Pro Forma
As Adjusted

 
  (unaudited)
(in thousands)

Balance Sheet Data:          
Cash and cash equivalents   $ 34,854    
Working capital     15,693    
Total assets     38,124    
Notes payable     8,074    
Preferred stock warrant liability     845    
Convertible preferred stock     37,637    
Accumulated deficit     (48,413 )  
Total stockholders' equity (deficit)     (47,662 )  

        The pro forma as adjusted balance sheet data reflects the (i) conversion of all of our outstanding shares of convertible preferred stock into 40,842,356 shares of common stock, (ii) sale of                         shares of common stock in this offering at the assumed initial public offering price of $            per share, after deducting the underwriting discounts and commissions and estimated offering expenses payable by us and (iii) sale of                         shares of common stock and                          shares of common stock in concurrent private placements to Schering-Plough and GSK, respectively, at the assumed initial public offering price of $             per share.

        A $1.00 increase (decrease) in the assumed initial public offering price of $    per share would increase (decrease) each of cash and cash equivalents, working capital, total assets and total stockholders' equity by approximately $     million, assuming that the number of shares offered by us, as set forth on the cover page of this prospectus, remains the same and after deducting estimated underwriting discounts and commissions and any estimated offering expenses payable by us.

8



RISK FACTORS

         Investing in our common stock involves a high degree of risk. You should carefully consider the following risk factors, as well as the other information in this prospectus, before deciding whether to invest in shares of our common stock. The occurrence of any of the following adverse developments described in the following risk factors could harm our business, financial condition, results of operations or prospects. In that case, the trading price of our common stock could decline, and you may lose all or part of your investment.

Risks Relating to the Development, Regulatory Approval and Commercialization of Our Product Candidates

         We are largely dependent on the regulatory approval of our most advanced product candidates, especially AN2690, and we cannot be certain that these product candidates will receive regulatory approval.

        We have invested a significant portion of our efforts and financial resources in the development of our most advanced product candidates, especially AN2690, which is currently in clinical trials for the treatment of onychomycosis. Our ability to generate revenue related to product sales, which we do not expect will occur for at least the next several years, if ever, will depend on the successful development and regulatory approval of our product candidates. We entered into a license, development and commercialization agreement with Schering-Plough in February 2007, pursuant to which Schering-Plough is responsible for Phase 3 clinical trials, regulatory approval and commercialization of AN2690. If Schering-Plough is not able to obtain regulatory approval for AN2690 or the milestones set forth in the agreement are not achieved or if Schering-Plough terminates our agreement, we may not be able to commercialize AN2690. In addition, our clinical development programs for our other product candidates may not lead to regulatory approval from the FDA and similar foreign regulatory agencies and we may therefore fail to commercialize those product candidates. Any failure to obtain regulatory approvals would have a material and adverse effect on our business.

        We currently have no approved products for sale and we cannot guarantee that we will ever have marketable products. The research, testing, manufacturing, labeling, approval, selling, marketing and distribution of products are subject to extensive regulation by the FDA and other regulatory authorities in the United States and other countries, with regulations differing from country to country. We are not permitted to market our product candidates in the United States until we receive approval of a new drug application, or NDA, from the FDA. We have not submitted an NDA for any of our product candidates. Obtaining approval of an NDA is a lengthy, expensive and uncertain process.

         Delays in the commencement, enrollment and completion of clinical trials could result in increased costs to us and delay or limit our ability to obtain regulatory approval for our product candidates.

        Delays in the commencement, enrollment and completion of clinical trials could increase our product development costs and hinder our ability to commence marketing our product candidates. We do not know whether Schering-Plough will commence Phase 3 clinical trials for AN2690 as planned or whether these trials will be completed on schedule, if at all. In particular, the timing of commencement of Phase 3 clinical trials for AN2690 is subject to satisfactory completion of certain non-clinical testing of the product candidate. The outcome of such testing could delay commencement of the Phase 3 clinical trials beyond the end of 2008. In addition, we do not know whether planned clinical trials for our other most advanced product candidates will begin on time or will be completed on schedule or at all. The commencement and completion of clinical trials requires us, Schering-Plough, GSK or our potential future partners to identify and maintain a sufficient number of trial sites, many of which may already be engaged in other clinical trial programs for the same indication as our product candidates. Clinical trial sites may also be required to withdraw from a clinical trial as a result of changing standards of care or may otherwise become ineligible

9



to participate in our clinical trials. The commencement, enrollment and completion of clinical trials can be delayed for a variety of other reasons, including delays related to:

        In addition, a clinical trial may be suspended or terminated by us, our partners, the FDA or other regulatory authorities due to a number of factors, including:

        If we or our partners are required to conduct additional clinical trials or other testing of our product candidates beyond those that we currently contemplate, we may be delayed in obtaining, or may not be able to obtain, marketing approval for these product candidates. In addition, our partners may suspend or terminate their development and commercialization efforts, including clinical trials for our product candidates, at any time.

        Changes in regulatory requirements and guidance may occur and we or our partners may need to amend clinical trial protocols to reflect these changes with appropriate regulatory authorities. Amendments may require us or our partners to resubmit our clinical trial protocols to IRBs for re-examination, which may impact the costs, timing or successful completion of a clinical trial. If we or our partners experience delays in the completion of, or if we or our partners terminate, our clinical trials, the commercial prospects for our product candidates will be harmed, and our ability to generate revenue from sales of our products will be delayed. In addition, many of the factors that cause, or lead to, a delay in the commencement or completion of clinical trials may also ultimately lead to the denial of regulatory approval of a product candidate.

         Clinical failure can occur at any stage of clinical development. Because the results of earlier clinical trials are not necessarily predictive of future results, any product candidate we, Schering-Plough, GSK or our potential future partners advance through clinical trials may not have favorable results in later clinical trials or receive regulatory approval.

        Clinical failure can occur at any stage of our clinical development. Clinical trials may produce negative or inconclusive results, and we or our partners may decide, or regulators may require us, to conduct

10



additional clinical or non-clinical testing. Success in preclinical testing and early clinical trials does not ensure that later clinical trials will generate adequate data to demonstrate the efficacy and safety of a product candidate. If the results of ongoing or future clinical trials of AN2690 do not demonstrate expected safety or efficacy, including over a longer treatment period, the prospects for commercialization of AN2690 would be adversely affected. A number of companies in the pharmaceutical industry, including those with greater resources and experience than us, have suffered significant setbacks in Phase 3 clinical trials, even after seeing promising results in earlier clinical trials.

        Pending discussions with the FDA and the outcome of certain non-clinical testing of AN2690, we currently anticipate that Schering-Plough will initiate Phase 3 clinical trials for AN2690 by the end of 2008. The data collected from our previous clinical trials is not adequate to support regulatory approval of AN2690 or any of our other product candidates. Despite the results reported in earlier clinical trials for our product candidates, we do not know whether any Phase 2, Phase 3 or other clinical trials we or our partners may conduct will demonstrate adequate efficacy and safety to obtain regulatory approval to market our product candidates. In particular, changes in study protocols from Phase 2 clinical trials to Phase 3 clinical trials, such as an expected increase in the period of treatment for AN2690 or differences in study populations, could result in side effects or changes in efficacy that were not seen in earlier trials, as well as a higher rate of drop-out among clinical trial participants.

        Furthermore, additional safety studies are required for AN2690 and our other product candidates prior to submission of an NDA. If AN2690 or our other product candidates are found unsafe, they will not be commercialized and our business would be harmed.

         Our product candidates may have undesirable side effects which may delay or prevent marketing approval or, if approval is received, require them to be taken off the market or otherwise limit their sales.

        A small number of patients who received AN2690 treatment experienced skin irritation around their toenails during clinical trials of AN2690 for onychomycosis. These side effects were reversible and did not interrupt or delay our clinical trials. However, the results of future clinical trials may show that our product candidates may cause more severe skin irritation or other undesirable side effects, which could interrupt, delay or halt clinical trials, resulting in delay of, or failure to obtain, marketing approval from the FDA and other regulatory authorities. If any of our product candidates receives marketing approval and we or others later identify undesirable side effects caused by such products:


        Any of these events could prevent us, Schering-Plough, GSK or our potential future partners from achieving or maintaining market acceptance of the affected product or could substantially increase commercialization costs and expenses, which in turn could delay or prevent us from generating significant revenues from the sale of our product candidates.

11


         Increased scrutiny of clinical trials by regulatory agencies may delay or prevent marketing approval of our product candidates.

        In light of widely publicized events concerning the safety risk of certain drug products, regulatory authorities, members of Congress, the Government Accounting Office, medical professionals and the general public have raised concerns about potential drug safety issues. These events have resulted in the withdrawal of drug products, revisions to drug labeling that further limit use of the drug products and establishment of risk management programs that may, for instance, restrict distribution of drug products. The increased attention to drug safety issues may result in a more cautious approach by the FDA to clinical trials. Data from clinical trials may receive greater scrutiny with respect to safety, which may make the FDA or other regulatory authorities more likely to terminate clinical trials before completion, or require longer or additional clinical trials that may result in substantial additional expense and a delay or failure in obtaining approval or result in approval for a more limited indication than originally sought. Failure to adequately demonstrate the efficacy and safety of AN2690 or any of our other product candidates would prevent regulatory approval and, ultimately, the commercialization of that product candidate.

         All of our products in development require regulatory review and approval prior to commercialization. Any delay in the regulatory review or approval of any of our products in development will harm our business.

        All of our products in development require regulatory review and approval prior to commercialization. Any delays in the regulatory review or approval of our products in development would delay market launch, increase our cash requirements, increase the volatility of our stock price and result in additional operating losses.

        The process of obtaining FDA and other required regulatory approvals, including foreign approvals, often takes many years and can vary substantially based upon the type, complexity and novelty of the products involved. Furthermore, this approval process is extremely complex, expensive and uncertain. We, Schering-Plough, GSK or our potential future partners may be unable to submit any NDA in the United States or any marketing approval application or other foreign applications for any of our products. If we or our partners submit any NDA, including any amended NDA or supplemental NDA, to the FDA seeking marketing approval for any of our product candidates, the FDA must decide whether to either accept or reject the submission for filing. We cannot be certain that any of these submissions will be accepted for filing and reviewed by the FDA, or that the marketing approval application submissions to any other regulatory authorities will be accepted for filing and review by those authorities. We cannot be certain that we or our partners will be able to respond to any regulatory requests during the review period in a timely manner without delaying potential regulatory action. We also cannot be certain that any of our products will receive favorable recommendation from any FDA advisory committee or foreign regulatory bodies or be approved for marketing by the FDA or foreign regulatory authorities. In addition, delays in approvals or rejections of marketing applications may be based upon many factors, including regulatory requests for additional analyses, reports, data and studies, regulatory questions regarding data and results, changes in regulatory policy during the period of product development and the emergence of new information regarding our product candidates or other products.

        Data obtained from preclinical studies and clinical trials are subject to different interpretations, which could delay, limit or prevent regulatory review or approval of any of our product candidates. In addition, as a routine part of the evaluation of any potential drug, clinical trials are generally conducted to assess the potential for drug-to-drug interactions that could impact potential product safety. To date, we and our partners have not been requested to perform drug-to-drug interaction studies on our product candidates, but any such request may delay any potential product approval and will increase the expenses associated with clinical programs. Furthermore, regulatory attitudes towards the data and results required to demonstrate safety and efficacy can change over time and can be affected by many factors, such as the emergence of new information, including on other products, policy changes and agency funding, staffing

12



and leadership. We do not know whether future changes to the regulatory environment will be favorable or unfavorable to our business prospects.

        In addition, the environment in which our regulatory submissions may be reviewed changes over time. For example, average review times at the FDA for marketing approval applications have fluctuated over the last ten years, and we cannot predict the review time for any of our submissions with any regulatory authorities. In addition, review times can be affected by a variety of factors, including budget and funding levels and statutory, regulatory and policy changes.

         Our use of boron chemistry to develop pharmaceutical product candidates is novel and may not prove successful in producing approved products. Undesirable side effects of any of our product candidates, or of boron-based drugs developed by others, could prevent us from obtaining regulatory approval for our product candidates, extend the time period required to obtain regulatory approval or harm market acceptance of our product candidates, if approved.

        All of our product development activities are centered around compounds containing boron. The use of boron chemistry to develop new drugs is largely unproven. The only FDA-approved boron-based pharmaceutical product, Velcade, is an anticancer chemotherapy agent that has significant adverse side effects. We believe that the adverse side effects associated with Velcade are due to its unique mechanism of action. None of our product candidates or research activities employs the same mechanism of action as Velcade. Nonetheless, if potential patients, regulatory authorities, third-party payors or medical providers associate the adverse side effects of Velcade or other boron-based therapeutics that may be developed with all potential boron-based therapies, the market for our products could be adversely affected.

        Additionally, there can be no assurance that our product candidates will be free of adverse side effects. For example, a small number of our patients who received AN2690 treatment experienced reversible skin irritation around their toe nails during clinical trials of AN2690 for onychomycosis. Also, our preclinical and clinical safety studies to date have focused upon our product candidates for topical treatments and we have not conducted safety studies on potential side effects of systemic therapeutics using boron-based compounds, including those that may be developed pursuant to our collaboration with GSK. If boron-based drug treatments result in significant adverse side effects, they may not be useful as therapeutic agents. If we are unable to develop product candidates that are safe and effective using our boron chemistry platform, our business will be materially and adversely affected.

        Regulatory authorities may also require additional safety testing of boron-based compounds, which could delay the timing of and increase the cost for regulatory approvals of our product candidates. Even if topical treatments using our boron-based compounds do not have adverse side effects, systemic therapeutics might. Additionally, even if our boron-based compounds do not have adverse side effects but boron-based drugs developed by others do, it could affect the willingness of regulatory authorities, third-party payors and medical providers to approve, provide reimbursement for or use our boron-based drugs. If boron-based compounds prove unsuitable as therapeutic agents, our business will be significantly harmed.

         We have limited experience developing systemic therapeutics and may not be able to do so.

        Most of our drug discovery and clinical development efforts to date have focused upon the identification and development of boron-based topical treatments and all of our leading product candidates are topical treatments. Pursuant to our agreement with GSK, we will significantly increase our research and development efforts to identify boron-based compounds for use in systemic therapeutics. We have limited experience in the development and approval process for systemic therapeutics. Accordingly, it may take us longer or we may fail to develop a systemic product candidate, in which case we will not receive additional payments from GSK.

13



         If any of our product candidates for which we receive regulatory approval do not achieve broad market acceptance, the revenues that we generate from their sales will be limited.

        The commercial success of AN2690 or our other product candidates will depend upon the acceptance of these products among physicians, patients and the medical community. The degree of market acceptance of AN2690 or any of our other product candidates will depend on a number of factors, including:

        If our product candidates are approved, but do not achieve an adequate level of acceptance by physicians, health care payors and patients, we may not generate sufficient revenue from these products, and we may not become or remain profitable. In addition, our efforts to educate the medical community and third-party payors on the benefits of our product candidates may require significant resources and may never be successful. If our product candidates fail to achieve market acceptance after regulatory approval, we will not be able to generate significant revenue, if any.

         We have never marketed a drug before, and if we are unable to establish an effective sales force and marketing infrastructure, we may not be able to commercialize our product candidates successfully.

        We plan to market or co-promote our products in certain U.S. specialty markets. We currently do not have any internal sales, distribution and marketing capabilities. The development of a sales and marketing infrastructure for U.S. specialty markets will require substantial resources, will be expensive and time consuming and could negatively impact our commercialization efforts, including delay of any product launch. These costs may be incurred in advance of any approval of our product candidates. In addition, we may not be able to hire a sales force in the United States that is sufficient in size or has adequate expertise in the medical markets that we intend to target. If we are unable to establish our sales force and marketing capability, our operating results may be adversely affected.

         We expect that our existing and future product candidates will face competition and some of our competitors have significantly greater resources than us.

        The pharmaceutical industry is highly competitive, with a number of established, large pharmaceutical companies, as well as many smaller companies. Most of these companies have greater financial resources, marketing capabilities and experience in obtaining regulatory approvals for product candidates than us.

14



There are many pharmaceutical companies, biotechnology companies, public and private universities, government agencies and research organizations actively engaged in research and development of products that may target the same markets as our product candidates. We expect any future products we develop to compete on the basis of, among other things, product efficacy, price, extent of adverse side effects experienced and convenience of treatment procedures. One or more of our competitors may develop products based upon the principles underlying our proprietary technologies earlier than us, obtain approvals for such products from the FDA more rapidly than us or develop alternative products or therapies that are safer, more effective or more cost effective than any future products developed by us.

        The commercial opportunity for our product candidates could be significantly harmed if competitors are able to develop alternative formulations that compete with our product candidates. Compared to us, many of our potential competitors have substantially greater:

        As a result of these factors, our competitors may obtain regulatory approval of their products more rapidly than we are able to or may obtain patent protection or other intellectual property rights that limit our ability to develop or commercialize our product candidates. Our competitors may also develop drugs that are more effective, more widely-used and less costly than ours and may also be more successful than us in manufacturing and marketing their products.

         The dermatology market is competitive, which may adversely affect our ability to commercialize our dermatological product candidates.

        If approved for the treatment of onychomycosis, we anticipate that AN2690 would compete with other marketed nail fungal therapeutics including Lamisil, Sporanox, Penlac and generic versions of those compounds. AN2690 will also compete against over-the-counter products. If approved for the treatment of psoriasis, AN2728 will compete against Tazorac, vitamin D analogues and corticosteroids, as well as over-the-counter therapies. Certain of our other product candidates will, if they receive regulatory approval, compete against branded prescription drugs, generics or over-the-counter products. Even if a generic product or an over-the-counter product is less effective than our product candidates, a less effective generic or over-the-counter product may be more quickly adopted by health insurers and consumers than our competing product candidates based upon cost or convenience. In addition, each of our product candidates may compete against product candidates currently under development by other companies.

         Reimbursement decisions by third-party payors may have an adverse effect on pricing and market acceptance. If patients seek coverage or sufficient reimbursement for our products and are unable to obtain it, it is less likely that our products will be widely used.

        Successful commercialization of pharmaceutical products usually depends on the availability of adequate coverage and reimbursement from third-party payors. Patients or healthcare providers who purchase drugs generally rely on third-party payors to reimburse all or part of the costs associated with such products. Adequate coverage and reimbursement from governmental payors, such as Medicare and

15



Medicaid, and commercial payors, such as HMOs and insurance companies, can be central to new product acceptance.

        Current treatments for onychomycosis are often not reimbursed by third-party payors. We do not know the extent to which AN2690 will be reimbursed. Reimbursement decisions by third-party payors may have an effect on pricing and market acceptance. Our other leading product candidates, such as AN2728 for the treatment of psoriasis, are also subject to uncertain reimbursement decisions by third-party payors. Patients are less likely to use products if they do not receive adequate reimbursement.

        The market for our product candidates may depend on access to third-party payors' drug formularies, or lists of medications for which third-party payors provide coverage and reimbursement. Industry competition to be included in such formularies results in downward pricing pressures on pharmaceutical companies. Third-party payors may refuse to include a particular branded drug in their formularies when a competing generic product is available.

        All third-party payors, whether governmental or commercial, are developing increasingly sophisticated methods of controlling healthcare costs. In addition, in the United States, no uniform policy of coverage and reimbursement for medicines exists among all these payors. Therefore, coverage of and reimbursement for drugs can differ significantly from payor to payor and can be difficult and costly to obtain.

         We expect that a substantial portion of the market for our product candidates will be outside the United States. Even if our product candidates receive regulatory approval in the United States, we, Schering-Plough, GSK or our potential future partners may never receive approval or commercialize our product candidates outside of the United States.

        To market and commercialize any product candidates outside of the United States, we or our partners must establish and comply with numerous and varying regulatory requirements of other countries regarding safety and efficacy. Approval procedures vary among countries and can involve additional product testing and additional administrative review periods. The regulatory approval process in other countries may include all of the risks detailed above regarding FDA approval in the United States as well as other risks. Regulatory approval in one country does not ensure regulatory approval in another, but a failure or delay in obtaining regulatory approval in one country may have a negative effect on the regulatory process in others. Failure to obtain regulatory approval in other countries or any delay or setback in obtaining such approval could have the same adverse effects detailed above regarding FDA approval in the United States. As described above, such effects include the risks that our product candidates may not be approved for all indications requested, or at all, which could limit the uses of our product candidates and have an adverse effect on product sales and potential royalties, and that such approval may be subject to limitations on the indicated uses for which the product may be marketed or require costly, post-marketing follow-up studies.

         Even if our product candidates receive regulatory approval, we may still face future development and regulatory difficulties.

        Even if regulatory approval is obtained for any of our product candidates, regulatory authorities may still impose significant restrictions on a product's indicated uses or marketing or impose ongoing requirements for potentially costly post-approval studies. Given the number of recent high profile adverse safety events with certain drug products, regulatory authorities may require, as a condition of approval, costly risk management programs which may include safety surveillance, restricted distribution and use, patient education, enhanced labeling, expedited reporting of certain adverse events, pre-approval of promotional materials and restrictions on direct-to-consumer advertising. For example, any labeling approved for any of our product candidates may include a restriction on the term of its use, or it may not include one or more of our intended indications. Furthermore, in the United States, heightened Congressional scrutiny on the adequacy of the FDA's drug approval process and the agency's efforts to

16


assure the safety of marketed drugs has resulted in the proposal of new legislation addressing drug safety issues. If enacted, any new legislation could result in delays or increased costs during the period of product development, clinical trials and regulatory review and approval, as well as increased costs to assure compliance with any new post-approval regulatory requirements. Any of these restrictions or requirements could force us or our partners to conduct costly studies.

        Our product candidates will also be subject to ongoing regulatory requirements for the labeling, packaging, storage, advertising, promotion, record-keeping and submission of safety and other post-market information on the drug. In addition, approved products, manufacturers and manufacturers' facilities are subject to continual review and periodic inspections. If a regulatory agency discovers previously unknown problems with a product, such as adverse events of unanticipated severity or frequency, or problems with the facility where the product is manufactured, a regulatory agency may impose restrictions on that product or us, including requiring withdrawal of the product from the market. If our product candidates fail to comply with applicable regulatory requirements, such as current Good Manufacturing Practices, or cGMPs, a regulatory agency may:

         Our limited experience in regulatory affairs could delay or harm our ability to obtain regulatory approvals necessary to market our product candidates.

        We have limited experience in preparing, submitting and prosecuting regulatory filings, including NDAs and other applications necessary to gain regulatory approvals. As a result, we may require more time and incur greater costs than our competitors and may not succeed in obtaining regulatory approvals of products that we develop, license or acquire.

         Guidelines and recommendations published by various organizations may affect the use of our products.

        Government agencies may issue regulations and guidelines directly applicable to us, Schering-Plough, GSK or our potential future partners and our product candidates. In addition, professional societies, practice management groups, private health/science foundations, and organizations involved in various diseases from time to time publish guidelines or recommendations to the health care and patient communities. These various sorts of recommendations may relate to such matters as product usage, dosage, route of administration and use of related or competing therapies. Changes to these recommendations or other guidelines advocating alternative therapies could result in decreased use of our products, which may adversely affect our results of operations.

17



         We face potential product liability exposure, and if successful claims are brought against us, we may incur substantial liability for a product candidate and may have to limit its commercialization.

        The use of our product candidates in clinical trials and the sale of any products for which we may obtain marketing approval expose us to the risk of product liability claims. Product liability claims may be brought against us or our partners by participants enrolled in our clinical trials, patients, health care providers or others using, administering or selling our products. If we cannot successfully defend ourselves against any such claims, we would incur substantial liabilities. Regardless of merit or eventual outcome, product liability claims may result in:

        We have obtained limited product liability insurance coverage for our clinical trials domestically and in selected foreign countries where we are conducting clinical trials. Our coverage is currently limited to $3 million per occurrence and $3 million in the aggregate per year. As such, our insurance coverage may not reimburse us or may not be sufficient to reimburse us for any expenses or losses we may suffer. Moreover, insurance coverage is becoming increasingly expensive, and, in the future, we may not be able to maintain insurance coverage at a reasonable cost or in sufficient amounts to protect us against losses due to product liability. We intend to expand our insurance coverage for products to include the sale of commercial products if we obtain marketing approval for our product candidates in development, but we may be unable to obtain commercially reasonable product liability insurance for any products approved for marketing. Large judgments have been awarded in class action lawsuits based on drugs that had unanticipated side effects. A successful product liability claim or series of claims brought against us could cause our stock price to fall and, if judgments exceed our insurance coverage, could decrease our cash and adversely affect our business.

         Our operations involve hazardous materials, which could subject us to significant liabilities.

        Our research and development processes involve the controlled use of hazardous materials, including chemicals. Our operations produce hazardous waste products. We cannot eliminate the risk of accidental contamination or discharge or injury from these materials. Federal, state and local laws and regulations govern the use, manufacture, storage, handling and disposal of these materials. We could be subject to civil damages in the event of exposure of individuals to hazardous materials. In addition, claimants may sue us for injury or contamination that results from our use of these materials and our liability may exceed our total assets. We maintain insurance for the use of hazardous materials. Our commercial business insurance covers us for up to $1 million per occurrence and up to $2 million in the aggregate per year and includes hazardous materials coverage. Our umbrella policy covers us for up to an additional $2 million per occurrence and up to $2 million in the aggregate per year. This coverage may not be adequate to cover all claims. Compliance with environmental and other laws and regulations may be expensive and current or future regulations may impair our research, development or production efforts.

18



         Our insurance policies are expensive and protect us only from some business risks, which will leave us exposed to significant uninsured liabilities.

        We do not carry insurance for all categories of risk that our business may encounter. For example, we do not carry earthquake insurance. In the event of a major earthquake in our region, our business could suffer significant and uninsured damage and loss. Some of the policies we currently maintain include general liability, employment practices liability, property, auto, workers' compensation, products liability and directors' and officers' insurance. We do not know, however, if we will be able to maintain existing insurance with adequate levels of coverage. Any significant uninsured liability may require us to pay substantial amounts, which would adversely affect our cash position and results of operations.

Risks Relating to Our Financial Position and Need for Additional Capital

         We have never been profitable. Currently, we have no products approved for commercial sale, and to date we have not generated any revenue from product sales. As a result, our ability to curtail our losses and reach profitability is unproven, and we may never achieve or sustain profitability.

        Our ability to reach profitability depends upon many factors including successful execution of our partnering strategy, continuing participation by Schering-Plough in the development and commercialization of AN2690, our ability to achieve research and development milestones for systemic therapeutics pursuant to our agreement with GSK and our ability to meet timing and cost targets. We have incurred significant net losses in each year since our inception, including net losses of approximately $5.2 million, $16.4 million and $19.6 million for 2004, 2005 and 2006, respectively. For the six months ended June 30, 2007, we incurred a net loss of $5.4 million, and as of June 30, 2007, we had an accumulated deficit of approximately $48.4 million. We have devoted most of our financial resources to research and development, including our preclinical development activities and clinical trials. None of our product candidates have been commercialized and we have therefore not generated any revenues from product sales. We expect to continue to incur increased expenses as we expand our research and development programs and advance our product candidates. For example, our research and development collaboration with GSK will require us to commit specific resources to discovery and development activities and will significantly increase our level of research and development expenditures on systemic drug discovery projects. We also expect an increase in our expenses associated with preparing for commercialization of our product candidates and creating additional infrastructure to support operations as a public company. As a result of the foregoing, we expect to continue to experience net losses and negative cash flows for the foreseeable future. In addition, if our alliances with Schering-Plough and GSK are unsuccessful or if we are unable to generate revenue from additional collaborations, then our losses and negative cash flows will be even greater.

        Because of the numerous risks and uncertainties associated with pharmaceutical product development, we are unable to accurately predict the timing or amount of increased expenses or when, or if, we will be able to achieve or maintain profitability. In addition, our expenses could increase beyond expectations if we are required by the FDA to perform studies in addition to those that we currently anticipate. To date, we have financed our operations primarily through the sale of equity securities, debt arrangements, government contracts and grants and the up-front payments under our agreements with Schering-Plough. The size of our future net losses will depend, in part, on the rate of future growth of our expenses and our ability to generate revenues. Revenues from our strategic alliances with Schering-Plough and GSK are uncertain because agreed-upon milestones may not be achieved, and AN2690 and product candidates that may be identified pursuant to our collaboration with GSK may not receive regulatory approval or, if approved, be accepted in the market. In addition, we may not be able to enter into other alliances and collaborations. If our product candidates are not successfully developed or commercialized, or if revenues from any product candidate that receives marketing approval are insufficient, we will not achieve profitability. Even if we do achieve profitability, we may not be able to sustain or increase profitability.

19



         We have a limited operating history and we expect a number of factors to cause our operating results to fluctuate on a quarterly and annual basis, which may make it difficult to predict our future performance.

        Our operations to date have been primarily limited to organizing and staffing our company, developing our technology and undertaking preclinical studies and clinical trials of our product candidates for topical treatments. We have not yet obtained regulatory approvals for any of our product candidates. Consequently, any predictions you make about our future success or viability may not be as accurate as they could be if we had a longer operating history. Our financial condition and operating results have varied significantly in the past and will continue to fluctuate from quarter-to-quarter or year-to-year due to a variety of factors, many of which are beyond our control. Factors relating to our business that may contribute to these fluctuations include the risk factors set forth in this section, as well as other factors described elsewhere in this prospectus. Due to these various factors, the results of any prior quarterly or annual periods should not be relied upon as indications of our future operating performance.

         If we are unable to raise capital when needed, we would be forced to delay, reduce or eliminate our product development programs.

        Developing pharmaceutical products, including conducting preclinical studies and clinical trials, is expensive. We expect our research and development expenses to increase in connection with our ongoing activities, particularly as we advance the preclinical and clinical programs of our product candidates for topical treatments. In addition, pursuant to our research collaboration with GSK, we have committed to significantly expand our research and development efforts to identify systemic therapeutics, an area where we have not previously devoted significant resources. Under the GSK agreement, we are required to use reasonable efforts to identify and optimize product candidates and have committed to provide certain numbers of personnel and other resources under four drug development projects. If the FDA requires that we perform additional studies to those that we currently anticipate, our expenses could increase beyond our current expectations and the timing of any potential product approval may be delayed. We currently have no commitments or arrangements for any additional financing to fund the research and development of our product candidates other than contingent milestone or royalty payments from Schering-Plough and GSK, which we may not receive. We believe that the net proceeds from this offering, existing cash and cash equivalents and interest thereon will be sufficient to fund our projected operating requirements through at least December 31, 2008. However, we may need to raise substantial additional capital in the future to complete the development and commercialization of our product candidates.

        Until we can generate a sufficient amount of revenue from our products, if ever, we expect to finance future cash needs through public or private equity offerings, debt financings or corporate collaboration and licensing arrangements. Additional funds may not be available when we need them on terms that are acceptable to us, or at all. If adequate funds are not available, we may be required to delay, reduce the scope of or eliminate one or more of our research or development programs or our commercialization efforts. To the extent that we raise additional funds by issuing equity securities, our stockholders may experience additional dilution, and debt financing, if available, may involve restrictive covenants. To the extent that we raise additional funds through collaboration and licensing arrangements, it may be necessary to relinquish some rights to our technologies or our product candidates or grant licenses on terms that may not be favorable to us. We may seek to access the public or private capital markets whenever conditions are favorable, even if we do not have an immediate need for additional capital at that time.

        Our future funding requirements will depend on many factors, including, but not limited to:

20


Risks Related to Our Dependence on Third Parties

         We are dependent upon Schering-Plough to develop, manufacture and commercialize our lead product candidate, AN2690.

        In February 2007, we entered into an exclusive license, development and commercialization agreement with Schering-Plough for the development and worldwide commercialization of our lead product candidate, AN2690. Under the agreement, Schering-Plough assumed sole responsibility for development, regulatory approval and commercialization of AN2690. Although we retained the option, subject to certain conditions, to co-promote AN2690 to dermatologists in the United States for the treatment of onychomycosis, Schering-Plough retains control over commercialization decisions, including pricing, marketing, strategy and sales. Any future payments from Schering-Plough, including milestone and royalty payments to us, will depend on the extent to which AN2690 advances through development, regulatory approval and commercialization.

        With respect to control over decisions and responsibilities, the agreement provides for a joint steering committee and a joint commercialization committee, consisting of representatives of Schering-Plough and us. Ultimate decision-making authority as to matters within the collaboration, however, is vested in Schering-Plough. For example, we currently expect Schering-Plough to initiate Phase 3 clinical trials of AN2690 in onychomycosis by the end of 2008. However, Schering-Plough is not obligated to do so, and may delay such trials for a variety of reasons. Schering-Plough retains the right to terminate the agreement on a country-by-country basis on 180-days prior written notice to us, provided that termination with respect to the United States will terminate the license in its entirety and termination in certain countries may terminate the license with respect to an entire region.

        Our ability to receive any significant milestone and royalty revenue from AN2690 depends on the efforts of Schering-Plough. If AN2690 receives regulatory approval we will be largely dependent on Schering-Plough to market it. If Schering-Plough does not devote sufficient resources to market AN2690 or is ineffective in doing so, our operating results will be materially and adversely affected. We cannot assure you that Schering-Plough will fulfill its obligations under this agreement or develop and commercialize AN2690. If Schering-Plough fails to fulfill its obligations under this agreement or terminates the agreement, we would need to obtain the capital necessary to fund the development and commercialization of AN2690 or enter into alternative arrangements with a third party. We could also become involved in disputes with Schering-Plough, which could lead to delays in or termination of development and commercialization of AN2690 and time-consuming and expensive litigation or arbitration. If Schering-Plough terminates or breaches the agreement with us or otherwise does not advance AN2690, the chances of successfully developing or commercializing AN2690 would be materially and adversely affected.

         We expect to expend substantial resources in our collaboration with GSK. If the research collaboration fails to successfully identify product candidates or if GSK elects not to license any of the resulting compounds or fails to

21



successfully develop and commercialize any compounds it does license, our operating results and financial condition will be materially and adversely affected.

        In October 2007, we entered into a research and development collaboration, option and license agreement with GSK for the discovery, development, manufacture and worldwide commercialization of novel systemic therapeutics for viral and bacterial diseases utilizing our boron-based chemistry. During the research term, both we and GSK are committed to use our reasonable efforts to discover and optimize compounds and to provide specified resources, including certain numbers of full-time equivalent scientists, on a project-by-project basis. Each party is responsible for its own research costs and we expect to expend substantial resources on the collaboration. If we fail to successfully identify product candidates or demonstrate proof of concept for the candidates we identify, our operating results and financial condition will be materially and adversely affected. GSK has the right, but is not required, to exclusively license a specified number of compounds under the agreement. GSK is obligated to make payments to us upon the achievement of certain initial discovery and developmental milestones but further, more significant milestone payments are payable only on compounds that GSK chooses to license. Accordingly, achievement of future payments from GSK depends upon the extent to which the collaborative research projects successfully identify compounds that meet agreed upon criteria and GSK chooses to license such compounds for further development and commercialization. If we devote substantial resources to a research project and GSK elects not to exercise its option with respect to any resulting product candidates, our financial condition will be materially and adversely affected.

        If GSK elects to license a compound, GSK will assume sole responsibility for development, regulatory approval and commercialization of such compound. Accordingly, even with respect to compounds that GSK chooses to license, if any, future payments from GSK, including milestone and royalty payments to us, will depend on the extent to which such licensed compounds advance through development, regulatory approval and commercialization. Additionally, GSK can choose to terminate the agreement on six months' notice or its license to any compounds at any time with no further obligation to develop and commercialize such compounds. Although we retain rights to develop and market compounds that GSK does not license or if GSK terminates the agreement or a license, we would not be eligible to receive further payments from GSK for the affected compounds and would be required to fund further development and commercialization ourselves or with other partners if we continue to pursue the product candidate.

        With respect to control over decisions and responsibilities, the agreement provides for a joint research committee to oversee the research collaboration consisting of representatives of GSK and us. Decisions regarding projects will be made on a consensus basis, except that ultimate decision-making authority with respect to the design of proof of concept trials for each research compound and determining whether proof of concept criteria have been satisfied is vested in GSK.

        If GSK does not devote sufficient resources to the research, development and commercialization of compounds identified through our research collaboration or is ineffective in doing so, our operating results will be materially and adversely affected. In particular, under the agreement, GSK is generally entitled to, either alone or with third parties, develop and commercialize compounds directed at the same targets we are working on under the agreement. If GSK independently develops compounds that compete with our compounds, it could elect to advance such compounds and not develop or commercialize our product candidates. We cannot assure you that GSK will fulfill its obligations under this agreement or develop and commercialize compounds identified by the research collaboration. If GSK fails to fulfill its obligations under this agreement or terminates the agreement, we would need to obtain the capital necessary to fund the development and commercialization of such compounds, enter into alternative arrangements with a third party or halt our development efforts in these areas. We could also become involved in disputes with GSK, which could lead to delays in or termination of the research collaboration or the development and commercialization of identified product candidates and time-consuming and expensive litigation or arbitration. If GSK terminates or breaches the agreement with us or otherwise does not advance the

22



compounds identified by our research collaboration, our chances of successfully developing or commercializing such compounds would be materially and adversely affected.

         We may not be successful in maintaining or establishing development and commercialization collaborations, which could adversely affect our ability to develop certain of our product candidates and our financial condition and operating results.

        Developing pharmaceutical products, conducting clinical trials, obtaining regulatory approval, establishing manufacturing capabilities and marketing approved products is expensive. Consequently, we have entered into an agreement with Schering-Plough for the development and commercialization of AN2690, and with GSK for the identification, development and commercialization of certain boron-based systemic product candidates, and we plan to establish alliances for development and commercialization of other product candidates and research programs. We expect to face competition in seeking appropriate collaborators. Moreover, collaboration arrangements are complex and time consuming to negotiate, document and implement and they may require substantial resources to maintain. We may not be successful in our efforts to establish and implement collaborations or other alternative arrangements for the development of our product candidates. When we partner with a third party for development and commercialization of a product candidate, we can expect to relinquish some or all of the control over the future success of that product candidate to the third party. The terms of any collaboration or other arrangement that we establish may not be favorable to us. In addition, any collaboration that we enter into may be unsuccessful in the development and commercialization of our product candidates. In some cases, we may be responsible for continuing preclinical and initial clinical development of a partnered product candidate or research program, and the payment we receive from our collaboration partner may be insufficient to cover the cost of this development. If we are unable to reach agreements with suitable collaborators for our product candidates we would face increased costs, we may be forced to limit the number of our product candidates we can commercially develop and we might fail to commercialize particular products or programs for which a suitable collaborator cannot be found. If we fail to achieve successful collaborations, our operating results and financial condition will be materially and adversely affected.

        Our strategy is to develop a marketing and sales force targeting dermatologists and other specialty markets in the United States. We expect that the collaborations we intend to establish with third parties for development and commercialization of our product candidates will include partnering for marketing and sales into primary care markets and for sales outside the United States. Our collaboration partner may not devote sufficient resources to the commercialization of our product candidates or may otherwise fail in their commercialization. If we are unable to establish effective collaborations to enable the sale of our product candidates to physicians and in geographical regions that will not be covered by our own marketing and sales force, or if our collaboration partners do not successfully commercialize our product candidates, then our ability to achieve revenues from product sales outside of U.S. dermatology and other specialty markets will be adversely affected.

         We depend on third-party contractors for a substantial portion of our operations and may not be able to control their work as effectively as if we performed these functions ourselves.

        Part of our strategy is to achieve operational efficiencies by outsourcing substantial portions of our operations to third-party service providers. We currently outsource certain functions including chemical synthesis, biological screening and manufacturing to a variety of different parties. Our agreements with third-party service providers and clinical research organizations are on a study-by-study basis and are typically short-term. Our agreements with chemical synthesis suppliers typically run from three months to one year. In all cases, we may terminate the agreements with notice and are responsible for the supplier's previously incurred costs.

        Because we have relied on third parties, our internal capacity to perform these functions is limited. Outsourcing these functions involves risk that third parties may not perform to our standards, may not

23



produce results in a timely manner or may fail to perform at all. In addition, the use of third-party service providers requires us to disclose our proprietary information to these parties, which could increase the risk that this information will be misappropriated. There are a limited number of third-party service providers that specialize or have the expertise required to achieve our business objectives. Identifying, qualifying and managing performance of third-party service providers can be difficult, time consuming and cause delays in our development programs. We currently have a small number of employees, which limits the internal resources we have available to identify and monitor our third-party providers. To the extent we are unable to identify, retain and successfully manage the performance of third-party service providers in the future, our business may be adversely affected.

         We have no experience manufacturing our product candidates on a large clinical-scale or commercial-scale and have no manufacturing facility. As a result, we are dependent on numerous third parties for the manufacture of our product candidates and our supply chain, and if we experience problems with any of these suppliers, the manufacturing of our products could be delayed.

        We do not own or operate facilities for the manufacture of our product candidates, which includes the drug substance and vehicle used to deliver the drug. We have limited personnel with experience in drug manufacturing. We currently outsource all manufacturing and packaging of our preclinical and clinical product candidates to third parties and intend to continue to do so. In addition, we do not currently have any agreements with third-party manufacturers for the long-term commercial supply of our product candidates. We may be unable to enter agreements for commercial supply with third-party manufacturers, or may be unable to do so on acceptable terms. We may not be able to establish additional sources of supply for our products. Such suppliers are subject to regulatory requirements, covering manufacturing, testing, quality control and record keeping relating to our product candidates, and subject to ongoing inspections by the regulatory agencies. Failure by any of our suppliers to comply with applicable regulations may result in long delays and interruptions to our product candidate supply while we seek to secure another supplier that meets all regulatory requirements.

        Reliance on third-party manufacturers entails risks to which we would not be subject if we manufactured the product candidates ourselves, including:

        Any of these factors could cause the delay of clinical trials, regulatory submissions, required approvals or commercialization of our products, cause us to incur higher costs and prevent us from commercializing our product candidates successfully. Furthermore, if our contract manufacturers fail to deliver the required commercial quantities of finished product on a timely basis and at commercially reasonable prices and we are unable to find one or more replacement manufacturers capable of production at a substantially equivalent cost, in substantially equivalent volumes and quality and on a timely basis, we would likely be unable to meet demand for our products and clinical trials may be delayed or we could lose potential revenue. It may take several years to establish an alternative source of supply for our product candidates and to have any such new source approved by the FDA.

        Schering-Plough will either manufacture AN2690 or will contract to have AN2690 manufactured by a third party. The transition of AN2690 production or the inability to manufacture or obtain sufficient supplies of the drug product or formulation could adversely effect clinical trial enrollment or timing or, if AN2690 is approved, product commercialization.

24



         If we lose our relationships with contract research organizations, our drug development efforts could be delayed.

        We are substantially dependent on third-party vendors and contract research organizations for preclinical studies and clinical trials related to our drug discovery and development efforts. If we lose our relationship with any one or more of these providers, we could experience a significant delay in both identifying another comparable provider and then contracting for its services, which could adversely affect our development efforts. We may be unable to retain an alternative provider on reasonable terms, if at all. Even if we locate an alternative provider, it is likely that this provider will need additional time to respond to our needs and may not provide the same type or level of services as the original provider. In addition, any contract research organization that we retain will be subject to the FDA's regulatory requirements and similar foreign standards and we do not have control over compliance with these regulations by these providers. Consequently, if these practices and standards are not adhered to by these providers, the development and commercialization of our product candidates could be delayed, which could severely harm our business and financial condition.

Risks Relating to Our Intellectual Property

         It is difficult and costly to protect our proprietary rights, and we may not be able to ensure their protection.

        Our commercial success will depend in part on obtaining and maintaining patent protection and trade secret protection of our current and future product candidates and the methods used to manufacture them, as well as successfully defending these patents against third-party challenges. Our ability to stop third parties from making, using, selling, offering to sell or importing our products is dependent upon the extent to which we have rights under valid and enforceable patents or trade secrets that cover these activities. In addition, while our patent applications covering AN2690 include claims for all relevant pharmaceutical uses of the compound, they do not include a claim for composition of matter for the AN2690 molecule due to the existence of prior art relating to a non-pharmaceutical use of the molecule. We currently own one issued patent, which was issued outside of the United States and there can be no assurance that our pending patent applications will result in issued patents. As of October 2, 2007, we are the owner of record and are actively pursuing 17 U.S. patent applications (3 provisional and 14 non-provisional), 6 international (PCT) patent applications and 94 non-U.S. patent applications in 16 jurisdictions, including the European Union, Japan, Canada, Australia and Mexico. Seven U.S. patent applications, 2 international PCT applications and 55 foreign applications are related to AN0128. Seven U.S. patent applications, 5 international PCT applications and 13 foreign applications are related to AN2690. Seven U.S. patent applications, 5 international PCT applications and 13 foreign applications are related to AN2718. Six U.S. patent applications, 5 international PCT applications and 13 foreign applications are related to AN2728. Unless and until such patents are issued, we may be unable to preclude others from working in the area in which we seek intellectual property protection pursuant to these patent applications.

        The patent positions of pharmaceutical and biopharmaceutical companies can be highly uncertain and involve complex legal and factual questions for which important legal principles remain unresolved. No consistent policy regarding the breadth of claims allowed in biopharmaceutical patents has emerged to date in the United States. The pharmaceutical patent situation outside the United States is even more uncertain. Changes in either the patent laws or in interpretations of patent laws in the United States and other countries may diminish the value of our intellectual property. Accordingly, we cannot predict the breadth of claims that may be allowed or enforced in the patents that may be issued from the applications we currently or may in the future own or license from third-parties. Further, if any patents we obtain or license are deemed invalid and unenforceable, it could impact our ability to commercialize or license our technology.

25



        The degree of future protection for our proprietary rights is uncertain because legal means afford only limited protection and may not adequately protect our rights or permit us to gain or keep our competitive advantage. For example:

        We also may rely on trade secrets to protect our technology, especially where we do not believe patent protection is appropriate or obtainable. However, trade secrets are difficult to protect. Although we use reasonable efforts to protect our trade secrets, our employees, consultants, contractors, outside scientific collaborators and other advisors may unintentionally or willfully disclose our information to competitors. Enforcing a claim that a third party illegally obtained and is using any of our trade secrets is expensive and time consuming, and the outcome is unpredictable. In addition, courts outside the United States, are sometimes less willing to protect trade secrets. Moreover, our competitors may independently develop equivalent knowledge, methods and know-how. Our patent applications would not prevent others from taking advantage of the chemical properties of boron to discover and develop new therapies, including therapies for the indications we are targeting. If others seek to develop boron-based therapies, their research and development efforts may inhibit our ability to conduct research in certain areas and expand our intellectual property portfolio.

         We may incur substantial costs as a result of litigation or other proceedings relating to patent and other intellectual property rights and we may be unable to protect our rights to, or use, our technology.

        If we choose to go to court to stop another party from using the inventions claimed in any patents we obtain, that individual or company has the right to ask the court to rule that such patents are invalid or should not be enforced against that third party. These lawsuits are expensive and would consume time and resources and divert the attention of managerial and scientific personnel even if we were successful in stopping the infringement of such patents. In addition, there is a risk that the court will decide that such patents are not valid and that we do not have the right to stop the other party from using the inventions. There is also the risk that, even if the validity of such patents is upheld, the court will refuse to stop the other party on the ground that such other party's activities do not infringe our rights to such patents. In addition, the U.S. Supreme Court has recently modified some tests used by the U.S. Patent Office in granting patents over the past 20 years, which may decrease the likelihood that we will be able to obtain patents and increase the likelihood of challenge of any patents we obtain or license.

        Furthermore, a third party may claim that we or our manufacturing or commercialization partners are using inventions covered by the third party's patent rights and may go to court to stop us from engaging in our normal operations and activities, including making or selling our product candidates. These lawsuits are costly and could affect our results of operations and divert the attention of managerial and scientific personnel. There is a risk that a court would decide that we or our commercialization partners are infringing the third party's patents and would order us or our partners to stop the activities covered by the patents. In that event, we or our commercialization partners may not have a viable way around the patent and may need to halt commercialization of the relevant product with it. In addition, there is a risk that a court will order us or our partners to pay the other party damages for having violated the other party's

26



patents. Under our agreement with Schering-Plough, we may be required to share in any license fees or royalty payments that Schering-Plough must pay arising from third-party claims of intellectual property infringement. In the future, we may agree to indemnify our commercial partners against certain intellectual property infringement claims brought by third parties. The pharmaceutical and biotechnology industries have produced a proliferation of patents, and it is not always clear to industry participants, including us, which patents cover various types of products or methods of use. The coverage of patents is subject to interpretation by the courts, and the interpretation is not always uniform. If we are sued for patent infringement, we would need to demonstrate that our products or methods either do not infringe the patent claims of the relevant patent or that the patent claims are invalid, and we may not be able to do this. Proving invalidity is difficult. For example, in the United States, proving invalidity requires a showing of clear and convincing evidence to overcome the presumption of validity enjoyed by issued patents.

        Because some patent applications in the United States may be maintained in secrecy until the patents are issued, because patent applications in the United States and many foreign jurisdictions are typically not published until eighteen months after filing, and because publications in the scientific literature often lag behind actual discoveries, we cannot be certain that others have not filed patent applications for technology covered by our pending applications, or that we were the first to invent the technology. Our competitors may have filed, and may in the future file, patent applications covering technology similar to ours. Any such patent application may have priority over our patent applications, which could further require us to obtain rights to issued patents covering such technologies. If another party has filed a U.S. patent application on inventions similar to ours, we may have to participate in an interference proceeding declared by the U.S. Patent and Trademark Office to determine priority of invention in the United States. The costs of these proceedings could be substantial, and it is possible that such efforts would be unsuccessful if unbeknownst to us, the other party had independently arrived at the same or similar invention prior to our own invention, resulting in a loss of our U.S. patent position with respect to such inventions.

        Some of our competitors may be able to sustain the costs of complex patent litigation more effectively than we can because they have substantially greater resources. In addition, any uncertainties resulting from the initiation and continuation of any litigation could have a material adverse effect on our ability to raise the funds necessary to continue our operations.

         We do not have exclusive rights to intellectual property we developed under U.S. federally funded research grants, and we could ultimately lose the rights we do have under certain circumstances.

        Some of our intellectual property rights, including those covering AN0128, were developed in the course of research funded by the U.S. government. As a result, the U.S. government may have certain rights to intellectual property embodied in our current or future products. Government rights in certain inventions developed under a government-funded program include a non-exclusive, non-transferable, irrevocable worldwide license to use inventions for any governmental purpose. In addition, the U.S. government has the right to require us to grant exclusive licenses to any of these inventions to a third party if they determine that: (i) adequate steps have not been taken to commercialize the invention; (ii) government action is necessary to meet public health or safety needs; or (iii) government action is necessary to meet requirements for public use under federal regulations. The U.S. government also has the right to take title to these inventions if we fail to disclose the invention to the government and fail to file an application to register the intellectual property within specified time limits. In addition, the U.S. government may acquire title in any country in which a patent application is not filed within specified time limits.

27



Risks Related to Employee Matters and Managing Growth

         We will need to expand our operations and increase the size of our company, and we may experience difficulties in managing growth.

        As we increase the number of product development programs we have underway and advance our product candidates through preclinical studies and clinical trials, we will need to increase our product development, scientific and administrative headcount to manage these programs. Additionally, our research collaboration with GSK commits us to provide a certain number of full-time equivalent employees to participate in the collaboration, which will result in a significant increase in our research and development headcount and expenses. We also share responsibility with GSK to oversee and manage the four research projects contemplated by the GSK agreement. Managing these expanding development programs will require additional personnel for coordinating and overseeing our third-party service providers. In addition, to meet our obligations as a public company, we will need to increase our general and administrative headcount. To support this growth in our operations, we expect to hire additional employees within the next twelve months. Our management, personnel and systems currently in place may not be adequate to support this future growth. We also expect to move into larger facilities in 2008. Our need to effectively manage our operations, growth and various projects requires that we:

        If we are unable to successfully manage this growth, our business may be adversely affected.

         We may not be able to manage our business effectively if we are unable to attract and retain key personnel.

        We may not be able to attract or retain qualified management, finance, scientific and clinical personnel in the future due to the intense competition for qualified personnel among biotechnology, pharmaceutical and other businesses, particularly in Northern California. If we are not able to attract and retain necessary personnel to accomplish our business objectives, we may experience constraints that will significantly impede the achievement of our development objectives, our ability to raise additional capital and our ability to implement our business strategy.

        Our industry has experienced a high rate of turnover of management personnel in recent years. We are highly dependent on the development, regulatory, commercialization and business development expertise of our executive officers and key employees identified in the "Management" section of this prospectus. If we lose one or more of our executive officers or key employees, our ability to implement our business strategy successfully could be seriously harmed. In August 2007, our board of directors approved the terms of a change of control and severance agreement that we will enter into with each of our executive officers and key employees as part of our retention efforts. The terms of these agreements, as well as the terms of our arrangements with our Chief Executive Officer and Chief Financial Officer, are described in the "Employment, Change of Control and Severance Agreements" section of this prospectus. Replacing executive officers and key employees may be difficult and may take an extended period of time because of the limited number of individuals in our industry with the breadth of skills and experience required to develop, gain regulatory approval of and commercialize products successfully. Competition to hire from this limited pool is intense, and we may be unable to hire, train, retain or motivate these additional key personnel. Our failure to retain key personnel could materially harm our business.

28



         Failure to effectively integrate our new officers into our organization could interfere with our management of our business and impair our ability to execute on our business strategy.

        Our Chief Business Officer and our Chief Financial Officer joined Anacor in May and June 2007, respectively. As a result, key members of our senior management team have not worked together as a group for a significant period of time. Our future performance will depend, in part on our ability to successfully integrate our newly hired officers into our management team and our ability to develop an effective working relationship among senior management. Our failure to integrate these individuals and create effective working relationships among them and other members of management could result in inefficiencies in the management of our business, harming our ability to execute our business strategy.

         Failure to make sufficient progress in building our finance infrastructure and improving our accounting systems and controls could impair our ability to comply with the financial reporting and internal controls requirements for publicly traded companies.

        We recently hired a Chief Financial Officer and are in the process of hiring additional finance personnel and building our financial infrastructure because we currently rely on consultants to perform certain of our accounting and financial reporting functions. To build this infrastructure, we will need to hire additional accounting and finance personnel and improve our accounting disclosure policies, procedures and controls. We are currently in the process of:

        As a public company, we will operate in an increasingly demanding regulatory environment which requires us to comply with the Sarbanes-Oxley Act of 2002 and the related rules and regulations of the Securities and Exchange Commission, expanded disclosure requirements, accelerated reporting requirements and more complex accounting rules. Company responsibilities required by the Sarbanes-Oxley Act include establishing corporate oversight and adequate internal control. As a result of our limited financial and administrative staffing and the need to establish basic financial infrastructure, we have only recently begun to prepare for the need to comply with Section 404 of the Sarbanes-Oxley Act, and we may be unable to do so on a timely basis. Because of the aforementioned factors, until we are able to expand our finance or administrative headcount or implement comprehensive accounting policies and procedures, we may not be able to prepare and disclose, in a timely manner, our financial statements and other required disclosures or comply with the Sarbanes-Oxley Act or existing or new reporting requirements.

         We may encounter unforeseen difficulties in the planned 2008 relocation of our facilities, which could disrupt our business operations or result in unplanned additional expenses.

        In October 2007 we entered into a facilities lease for a 36,960 square foot building consisting of office and laboratory space in Palo Alto, California, that will replace our current facility as our corporate headquarters. We expect the lease term to commence for the new facility in April 2008. The move to new facilities will involve the moving and installation of our laboratory and business equipment and the new facility may require more substantial upgrades than we anticipate. We will have to obtain necessary licenses and permits and make improvements before we can move into the new facility. We will also have to ensure that the facility we plan to vacate is safely cleaned and any hazardous materials are either safely moved or properly disposed of. Accordingly, the relocation could result in a temporary disruption to our business or cause us to incur unforeseen costs.

29



Risks Relating to Owning Our Common Stock

         After this offering, our executive officers, directors and principal stockholders will have the ability to control all matters submitted to our stockholders for approval.

        When this offering is completed, our executive officers, directors and stockholders who owned more than 5% of our outstanding common stock before this offering will, in the aggregate, beneficially own shares representing            % of our common stock assuming such persons do not purchase any shares of our common stock in this offering. As a result, if these stockholders were to choose to act together, they would be able to control all matters submitted to our stockholders for approval, as well as our management and affairs. For example, these persons, if they choose to act together, will control the election of directors and approval of any merger, consolidation, sale of all or substantially all of our assets or other business combination or reorganization. This concentration of voting power could delay or prevent an acquisition of us on terms that other stockholders may desire. The interests of this group of stockholders may not always coincide with your interests or the interests of other stockholders and they may act in a manner that advances their best interests and not necessarily those of other stockholders, including seeking a premium value for their common stock, and might affect the prevailing market price for our common stock.

         Our share price may be volatile and you may be unable to sell your shares at or above the offering price.

        The initial public offering price for our shares will be determined by negotiations between us and representatives of the underwriters and may not be indicative of prices that will prevail in the trading market. The market price of shares of our common stock could be subject to wide fluctuations in response to many risk factors listed in this section, and others beyond our control, including:


        Furthermore, the stock markets have experienced extreme price and volume fluctuations that have affected and continue to affect the market prices of equity securities of many companies. These fluctuations often have been unrelated or disproportionate to the operating performance of those companies. These broad market and industry fluctuations, as well as general economic, political and market conditions such as recessions, interest rate changes or international currency fluctuations, may negatively impact the market price of shares of our common stock. If the market price of shares of our common stock after this offering does not exceed the initial public offering price, you may not realize any return on your investment in us and may lose some or all of your investment.

30


         We may be subject to securities litigation, which is expensive and could divert management attention.

        In the past, companies that have experienced volatility in the market price of their stock have been subject to securities class action litigation. We may be the target of this type of litigation in the future. Securities litigation against us could result in substantial costs and divert our management's attention from other business concerns, which could seriously harm our business.

         No public market for our common stock currently exists and an active trading market may not develop or be sustained following this offering.

        Prior to this offering, there has been no public market for our common stock. An active trading market may not develop following the completion of this offering or, if developed, may not be sustained. The lack of an active market may impair your ability to sell your shares at the time you wish to sell them or at a price that you consider reasonable. The lack of an active market may also reduce the fair market value of your shares. An inactive market may also impair our ability to raise capital to continue to fund operations by selling shares and may impair our ability to acquire other companies or technologies by using our shares as consideration.

         If securities or industry analysts do not publish research or reports about our business, or publish negative reports about our business, our stock price and trading volume could decline.

        The trading market for our common stock will depend on the research and reports that securities or industry analysts publish about us or our business. We do not have any control over these analysts. There can be no assurance that analysts will cover us. If one or more of the analysts who cover us downgrade our stock or change their opinion of our stock, our stock price would likely decline. If one or more of these analysts cease coverage of our company or fail to regularly publish reports on us, we could lose visibility in the financial markets, which could cause our stock price or trading volume to decline.

         A significant portion of our total outstanding shares of common stock is restricted from immediate resale but may be sold into the market in the near future. This could cause the market price of our common stock to drop significantly, even if our business is doing well.

        Sales of a substantial number of shares of our common stock in the public market could occur in the future. These sales, or the perception in the market that the holders of a large number of shares of common stock intend to sell shares, could reduce the market price of our common stock. After this offering, we will have                        outstanding shares of common stock based on the number of shares outstanding as of June 30, 2007 and the concurrent private placements to Schering-Plough and GSK. Of these shares,                         may be resold in the public market immediately and the remaining                        shares are currently restricted under securities laws or as a result of lock-up agreements but will be able to be resold after the offering as described in the "Shares Eligible for Future Sale" section of this prospectus. Moreover, after this offering, holders of an aggregate of                        shares of our common stock will have rights, subject to some conditions, to require us to file registration statements covering their shares or to include their shares in registration statements that we may file for ourselves or other stockholders. We also intend to register all                        shares of common stock that we may issue under our equity compensation plans. Once we register these shares, they can be freely sold in the public market upon issuance and once vested, subject to the 180 day lock-up periods under the lock-up agreements described in the "Underwriting" section of this prospectus.

         Purchasers in this offering will experience immediate and substantial dilution in the book value of their investment.

        The initial public offering price will be substantially higher than the tangible book value per share of shares of our common stock based on the total value of our tangible assets less our total liabilities immediately following this offering. Therefore, if you purchase shares of our common stock in this offering, you will experience immediate and substantial dilution of approximately $            per share in the price you pay for shares of our common stock as compared to its tangible book value, assuming an initial

31



public offering price of $            per share and reflecting the concurrent private placements to Schering-Plough and GSK. To the extent outstanding options to purchase shares of common stock are exercised, there will be further dilution. Investors who purchase shares in this offering will contribute approximately      % of the total amount of equity capital raised by us through the date of this offering, but will only own approximately      % of the shares outstanding immediately following the completion of this offering and the two concurrent private placements. For further information on this calculation, see "Dilution" elsewhere in this prospectus.

         We have broad discretion in the use of net proceeds from this offering and may not use them effectively.

        Although we currently intend to use the net proceeds from this offering in the manner described in "Use of Proceeds" elsewhere in this prospectus, we will have broad discretion in the application of the net proceeds. Our failure to apply these funds effectively could affect our ability to continue to develop and eventually to manufacture and sell our products.

         Being a public company will increase our expenses and administrative burden.

        As a public company, we will incur significant legal, accounting and other expenses that we did not incur as a private company. In addition, our administrative staff will be required to perform additional tasks. For example, in anticipation of becoming a public company, we will need to adopt additional internal controls and disclosure controls and procedures, retain a transfer agent, adopt an insider trading policy and bear all of the internal and external costs of preparing and distributing periodic public reports in compliance with our obligations under the securities laws.

        In addition, changing laws, regulations and standards relating to corporate governance and public disclosure, including the Sarbanes-Oxley Act of 2002 and related regulations implemented by the Securities and Exchange Commission and the Nasdaq Global Market, are creating uncertainty for public companies, increasing legal and financial compliance costs and making some activities more time consuming. We are currently evaluating and monitoring developments with respect to new and proposed rules and cannot predict or estimate the amount of additional costs we may incur or the timing of such costs. These laws, regulations and standards are subject to varying interpretations, in many cases due to their lack of specificity, and, as a result, their application in practice may evolve over time as new guidance is provided by regulatory and governing bodies. This could result in continuing uncertainty regarding compliance matters and higher costs necessitated by ongoing revisions to disclosure and governance practices. We intend to invest resources to comply with evolving laws, regulations and standards, and this investment will result in increased general and administrative expenses and may divert management's time and attention from product development activities. If our efforts to comply with new laws, regulations and standards differ from the activities intended by regulatory or governing bodies due to ambiguities related to practice, regulatory authorities may initiate legal proceedings against us and our business may be harmed. In connection with this offering, we are increasing our directors' and officers' insurance coverage which will increase our insurance cost. In the future, it may be more expensive for us to obtain director and officer liability insurance, and we may be required to accept reduced coverage or incur substantially higher costs to obtain coverage. These factors could also make it more difficult for us to attract and retain qualified members of our board of directors, particularly to serve on our audit committee and compensation committee, and qualified executive officers.

         Anti-takeover provisions in our charter documents and under Delaware law could make an acquisition of us, which may be beneficial to our stockholders, more difficult and may prevent attempts by our stockholders to replace or remove our current management.

        Provisions in our amended and restated certificate of incorporation and our bylaws, both of which will become effective upon the completion of this offering, may delay or prevent an acquisition of us. In addition, these provisions may frustrate or prevent any attempts by our stockholders to replace or remove our current management by making it more difficult for stockholders to replace members of our board of directors, who are responsible for appointing the members of our management team. In addition, we are

32


governed by the provisions of Section 203 of the Delaware General Corporation Law, which prohibits, with some exceptions, stockholders owning in excess of 15% of our outstanding voting stock from merging or combining with us. Finally, our charter documents establish advanced notice requirements for nominations for election to our board of directors and for proposing matters that can be acted upon at stockholder meetings. Although we believe these provisions together provide for an opportunity to receive higher bids by requiring potential acquirers to negotiate with our board of directors, they would apply even if the offer may be considered beneficial by some stockholders.

33



SPECIAL NOTE REGARDING FORWARD-LOOKING STATEMENTS

        This prospectus contains forward-looking statements, including statements regarding the progress and timing of clinical trials, the safety and efficacy of our product candidates, actions to be taken by our partners, Schering-Plough and GSK, our ability to enter into additional alliances, our ability to scale and support commercial activities, the goals of our development activities, estimates of the potential markets for our product candidates, availability of drug product, availability of facilities to support our growth, our expected future revenues, operations and expenditures and projected cash needs. The forward-looking statements are contained principally in the sections entitled "Prospectus Summary," "Risk Factors," "Management's Discussion and Analysis of Financial Condition and Results of Operations" and "Business." These statements relate to future events or our future financial performance and involve known and unknown risks, uncertainties and other factors that could cause our actual results, levels of activity, performance or achievement to differ materially from those expressed or implied by these forward-looking statements.

        Forward-looking statements include all statements that are not historical facts. In some cases, you can identify forward-looking statements by terms such as "may," "will," "should," "could," "would," "expects," "plans," "anticipates," "believes," "estimates," "projects," "predicts," "potential," or the negative of those terms, and similar expressions and comparable terminology intended to identify forward-looking statements. These statements reflect our current views with respect to future events and are based on assumptions and subject to risks and uncertainties. Given these uncertainties, you should not place undue reliance on these forward-looking statements. These forward-looking statements represent our estimates and assumptions only as of the date of this prospectus and, except as required by law, we undertake no obligation to update or revise publicly any forward-looking statements, whether as a result of new information, future events or otherwise after the date of this prospectus. The forward-looking statements contained in this prospectus are excluded from the safe harbor protection provided by the Private Securities Litigation Reform Act of 1995 and Section 27A of the Securities Act of 1933, as amended, or the Securities Act.

34



USE OF PROCEEDS

        We estimate that we will receive net proceeds of approximately $             million from the sale of the shares of common stock offered in this offering, based on an assumed initial public offering price of $            per share (the mid-point of the price range set forth on the cover page of this prospectus) and after deducting the estimated underwriting discounts and commissions and estimated offering expenses payable by us. If the underwriters' over-allotment option is exercised in full, we estimate that our net proceeds will be approximately $             million. We will also receive $     million and $10 million from the sale of             and              shares of our common stock at the initial public offering price in concurrent private placements to Schering-Plough and GSK, respectively.

        A $1.00 increase (decrease) in the assumed initial public offering price of $            per share would increase (decrease) the net proceeds to us from this offering by $             million, assuming that the number of shares offered by us, as set forth on the cover page of this prospectus, remains the same and after deducting the estimated underwriting discounts and commissions and estimated offering expenses payable by us. Any changes in the initial public offering price will not change the net proceeds from our sale of common stock to Schering-Plough and GSK but will change the number of shares issued to Schering-Plough and GSK, respectively.

        We intend to use approximately $45.0 million of the net proceeds from this offering and the concurrent private placements to Schering-Plough and GSK to fund the following research and development activities:

        We intend to use the remainder of the net proceeds for working capital, capital expenditures and other general corporate purposes. We may also use a portion of the proceeds for the acquisition of, or investment in, technologies, products or companies that complement our business, although we have no current understandings, commitments or agreements to do so.

        Our expected use of net proceeds from this offering, together with the proceeds from the concurrent private placements of our common stock to Schering-Plough and GSK, represents our current intentions based upon our present plans and business condition. As of the date of this prospectus, we cannot predict with certainty all of the particular uses for the net proceeds to be received upon the completion of this offering or the amounts that we will actually spend on the uses set forth above. The amounts and timing of our actual use of net proceeds will vary depending on the relative success and cost of our research, preclinical and clinical development programs, and the amount and timing of revenues, if any, received from our collaborations with Schering-Plough and GSK and any other collaborations, among other factors. As a result, management will have broad discretion in the application of the net proceeds, and investors will be relying on our judgment regarding the application of the net proceeds of this offering.

        Until we use the net proceeds of this offering, we intend to invest the net proceeds in short-term, interest-bearing, investment-grade securities. We cannot predict whether the proceeds invested will yield a favorable return.

35



DIVIDEND POLICY

        We currently do not plan to declare dividends on shares of our common stock in the foreseeable future. We expect to retain our future earnings, if any, for use in the operation and expansion of our business. Subject to the foregoing, the payment of cash dividends in the future, if any, will be at the discretion of our board of directors and will depend upon such factors as earnings levels, capital requirements, our overall financial condition and any other factors deemed relevant by our board of directors. In addition, under the terms of our loan agreement, we may not pay dividends on our common stock without the consent of the lender.

36



CAPITALIZATION

        The following table sets forth our cash and cash equivalents and capitalization as of June 30, 2007:

        The pro forma as adjusted information below is illustrative only and our capitalization following the completion of this offering will be adjusted based on the actual initial public offering price. You should read this table together with "Management's Discussion and Analysis of Financial Condition and Results of Operations" and our financial statements and the related notes appearing elsewhere in this prospectus.

 
  As of June 30, 2007
 
  Actual
  Pro Forma
As Adjusted

 
  (unaudited)
(in thousands, except share and
per share data)

Cash and cash equivalents   $ 34,854   $  
   
 
Notes payable   $ 8,074   $  
Preferred stock warrant liability     845      
Convertible preferred stock, $0.001 par value; 40,255,601 shares authorized, 39,786,101 shares issued and outstanding, actual; no shares authorized, issued and outstanding, pro forma as adjusted     37,637      
Stockholders' equity (deficit):            
Preferred stock, $0.001 par value; no shares authorized, issued and outstanding, actual;                         shares authorized, no shares issued and outstanding, pro forma as adjusted            
Common stock, $0.001 par value; 55,150,000 shares authorized, 6,784,724 shares issued and outstanding, actual;                         shares authorized,                          shares issued and outstanding, pro forma as adjusted     7      
Additional paid-in capital     744      
Accumulated deficit     (48,413 )    
   
 
  Total stockholders' equity (deficit)     (47,662 )    
   
 
      Total capitalization   $ (1,106 ) $  
   
 

37


        The number of pro forma as adjusted shares of common stock shown as issued and outstanding in the table is based on the number of shares of our common stock outstanding as of June 30, 2007 and excludes:

        A $1.00 increase (decrease) in the assumed initial public offering price of $            per share would increase (decrease) each of cash and cash equivalents, total stockholders' equity and total capitalization by approximately $             million, assuming that the number of shares offered by us, as set forth on the cover page of this prospectus, remains the same and after deducting estimated underwriting discounts and commissions and estimated offering expenses payable by us. Any changes in the initial public offering price will not change the net proceeds from our sale of common stock to Schering-Plough and GSK, but will change the number of shares issued to Schering-Plough and GSK, respectively.

38



DILUTION

        Our pro forma net tangible book value as of June 30, 2007, was $             million, or $            per share of common stock. Pro forma net tangible book value per share represents the amount of our total tangible assets less our total liabilities, divided by the number of shares of common stock outstanding as of June 30, 2007, after giving effect to the conversion of all our convertible preferred stock into shares of our common stock.

        After giving effect to (i) the sale by us of                        shares of common stock in this offering at an assumed initial public offering price of $            per share, the midpoint of the range on the cover page of this prospectus, and after deducting underwriting discounts and commissions and estimated offering expenses payable by us, and (ii) the sale by us in the concurrent private placements of an aggregate of            shares of our common stock at the assumed initial public offering price, our pro forma as adjusted net tangible book value as of June 30, 2007, would have been approximately $             million, or approximately $            per share. This amount represents an immediate increase in net tangible book value of $            per share to our existing stockholders and an immediate dilution in net tangible book value of approximately $            per share to new investors purchasing shares of common stock in this offering. The following table illustrates this dilution on a per share basis:

Assumed initial public offering price per share         $  
  Pro forma net tangible book value as of June 30, 2007   $        
  Increase per share attributable to new investors            
   
     
Pro forma as adjusted net tangible book value per share after this offering            
         
Dilution in pro forma as adjusted net tangible book value per share to new investors         $  
         

        A $1.00 increase (decrease) in the assumed initial public offering price of $            per share would increase (decrease) our pro forma as adjusted net tangible book value as of June 30, 2007 by approximately $             million, assuming the number of shares offered by us, as set forth on the cover page of this prospectus, remains the same and after deducting estimated underwriting discounts and commissions and estimated offering expenses payable by us. A $1.00 increase in the assumed initial public offering price per share would also increase the pro forma as adjusted net tangible book value per share after this offering and the dilution in net tangible book value per share to new investors by $        and $        , respectively, assuming the number of shares offered by us, as set forth on the cover page of this prospectus, remains the same and after deducting estimated underwriting discounts and commissions and estimated offering expenses payable by us. A $1.00 decrease in the assumed initial public offering price per share would decrease the pro forma as adjusted net tangible book value per share after this offering and the dilution in net tangible book value per share to new investors by $        and $        , respectively, assuming the number of shares offered by us, as set forth on the cover page of this prospectus, remains the same and after deducting estimated underwriting discounts and commissions and estimated offering expenses payable by us. Because the dollar values of the concurrent private placement to Schering-Plough and GSK are fixed, changes in the assumed initial public offering price per share will change the number of shares to be outstanding after this offering. As such, changes in the resulting pro forma as adjusted net tangible book value per share after this offering and dilution in net tangible book value per share to new investors are not directly proportional to changes in the assumed initial public offering price per share.

        In addition, the above discussion and table assume no exercise of stock options after June 30, 2007. As of June 30, 2007 we had outstanding options to purchase a total of 4,676,003 shares of common stock at a weighted average exercise price of $0.49 per share. If all such options had been exercised as of June 30, 2007, pro forma as adjusted net tangible book value would be $            per share and dilution to new investors would be $            per share at the assumed initial public offering price.

39



        The following table summarizes, as of June 30, 2007, the differences between the number of shares purchased from us, the total consideration paid to us and the average price per share that existing stockholders and new investors paid. The table gives effect to the conversion of all of our convertible preferred stock into shares of our common stock and our private placements to Schering-Plough and GSK. The calculation below is based on an assumed initial public offering price of $            per share, the midpoint of the range on the cover page of this prospectus, and before deducting estimated underwriting discounts and commissions and estimated offering expenses that we must pay.

 
  Shares Purchased
  Total Consideration
   
 
  Average
Price
Per Share

 
  Number
  Percent
  Amount
  Percent
Existing stockholders before this offering         %            % $             
New investors                      
   
 
     
     
GSK                      
   
 
     
     
Schering-Plough                      
   
 
     
     
  Total       100 %     100 %    
   
 
     
     

        A $1.00 increase (decrease) in the assumed initial public offering price of $            per share would increase (decrease) total consideration paid by new investors and total consideration paid by all stockholders by $             million and $             million, respectively, assuming that the number of shares offered by us, as set forth on the cover page of this prospectus, remains the same and after deducting the estimated underwriting discounts and commissions and estimated offering expenses payable by us. Any changes in the initial public offering price will not change the net proceeds from our sale of common stock to Schering-Plough and GSK but will change the number of shares issued to Schering-Plough and GSK, respectively.

        If the underwriters exercise their over-allotment option in full, our existing stockholders would own    %, our new investors would own    %, Schering-Plough would own    %, and GSK would own    % of the total number of shares of our common stock outstanding after this offering.

        The above information assumes no exercise of stock options or the warrant outstanding as of June 30, 2007. As of June 30, 2007, there were:

40



SELECTED FINANCIAL DATA

        The following selected financial data should be read together with our financial statements and accompanying notes and "Management's Discussion and Analysis of Financial Condition and Results of Operations" appearing elsewhere in this prospectus. The selected financial data in this section is not intended to replace our financial statements and the accompanying notes. Our historical results are not necessarily indicative of our future results.

        The statements of operations data for 2002 and 2003 and the balance sheet data as of December 31, 2002, 2003 and 2004 were derived from our audited financial statements not included in this prospectus. The statements of operations data for 2004, 2005 and 2006 and the balance sheet data as of December 31, 2005 and 2006 were derived from our audited financial statements appearing elsewhere in this prospectus. The statements of operations data for the six months ended June 30, 2006 and 2007 and the balance sheet data as of June 30, 2007 have been derived from our unaudited condensed financial statements appearing elsewhere in this prospectus. The unaudited interim condensed financial statements have been prepared on the same basis as the annual financial statements and reflect all adjustments necessary to fairly state our financial position as of June 30, 2007 and results of operations for the six months ended June 30, 2006 and 2007.

 
  Year Ended December 31,
  Six Months
Ended June 30,

 
 
  2002
  2003
  2004
  2005
  2006
  2006
  2007
 
 
   
   
   
   
   
  (unaudited)

 
 
  (in thousands, except share and per share data)

 
Statement of Operations Data:                                            
Revenues   $ 1,935   $ 7,116   $ 7,052   $ 107   $ 861   $ 308   $ 9,320  
Operating expenses                                            
  Research and development     2,519     5,584     10,586     14,023     16,627     7,754     10,164  
  General and administrative     951     1,728     1,646     2,827     3,629     1,656     4,143  
   
 
 
 
 
 
 
 
    Total operating expenses     3,470     7,312     12,232     16,850     20,256     9,410     14,307  
   
 
 
 
 
 
 
 
Loss from operations     (1,535 )   (196 )   (5,180 )   (16,743 )   (19,395 )   (9,102 )   (4,987 )
Interest income     10     14     31     343     311     138     571  
Interest expense     (2 )   (44 )   (42 )   (44 )   (369 )       (649 )
Other expense                     (136 )       (301 )
   
 
 
 
 
 
 
 
Net loss   $ (1,527 ) $ (226 ) $ (5,191 ) $ (16,444 ) $ (19,589 ) $ (8,964 ) $ (5,366 )
   
 
 
 
 
 
 
 
Net loss per share—basic and diluted   $ (0.37 ) $ (0.05 ) $ (1.10 ) $ (3.18 ) $ (3.17 ) $ (1.52 ) $ (0.79 )
   
 
 
 
 
 
 
 
Weighted average shares outstanding used in calculating net loss per share—basic and diluted (1)     4,077,802     4,316,355     4,713,871     5,173,237     6,172,694     5,878,624     6,757,945  
Pro forma net loss per share—basic and diluted (1)                           $ (0.43 )       $ (0.11 )
                           
       
 
Pro forma weighted average shares outstanding used in calculating net loss per share—basic and diluted (1)                             45,706,365           47,600,305  

(1)
Please see Note 2 to our audited financial statements for an explanation of the method used to calculate basic and diluted net loss per common share attributable to common stockholders, the pro forma basic and diluted net loss per common share and the number of shares used in the computation of the per share amounts.

41


 
  As of December 31,
   
 
 
  As of June 30,
2007

 
 
  2002
  2003
  2004
  2005
  2006
 
 
   
   
   
   
   
  (unaudited)

 
 
  (in thousands)

 
Balance Sheet Data:                                      
Cash and cash equivalents   $ 1,471   $ 1,580   $ 1,275   $ 10,419   $ 5,236   $ 34,854  
Working capital     1,958     2,076     (257 )   8,332     2,848     15,693  
Total assets     2,721     4,305     2,413     11,565     6,517     38,124  
Notes payable         219             7,863     8,074  
Preferred stock warrant liability                     544     845  
Convertible preferred stock     3,793     4,767     7,765     32,602     37,637     37,637  
Accumulated deficit     (1,596 )   (1,823 )   (7,014 )   (23,458 )   (43,047 )   (48,413 )
Total stockholders' equity (deficit)     (1,578 )   (1,792 )   (6,949 )   (23,332 )   (42,530 )   (47,662 )

42



MANAGEMENT'S DISCUSSION AND ANALYSIS OF FINANCIAL CONDITION AND
RESULTS OF OPERATIONS

         You should read the following discussion and analysis together with our financial statements and the notes to those statements included elsewhere in this prospectus. This discussion contains forward-looking statements that involve risks and uncertainties. As a result of many factors, such as those set forth under "Risk Factors" and elsewhere in this prospectus, our actual results may differ materially from those anticipated in these forward-looking statements.

Overview

        We are a biopharmaceutical company developing novel small-molecule therapeutics derived from our boron chemistry platform. We believe that our expertise in creating new boron-based compounds enables us to develop proprietary product candidates rapidly and cost-effectively that address unmet medical needs across many therapeutic areas. We have focused initially on developing topical applications of our compounds to treat fungal, bacterial and inflammatory diseases. We believe topical therapeutics generally have lower development costs, reduced risk of side effects and faster time to market than systemic therapeutics. Our most advanced product candidate is AN2690, a novel topical antifungal in development for the treatment of onychomycosis, a fungal infection of the nail and nail bed. In addition, we have a portfolio of other topical product candidates in development for the treatment of psoriasis, gingivitis, acne, vaginal candidiasis, or yeast infections, and tinea pedis, or athlete's foot.

        In February 2007, we entered into an exclusive license, development and commercialization agreement with Schering-Plough for the development and worldwide commercialization of AN2690 for all indications, including the treatment of onychomycosis. Pursuant to the agreement, Schering-Plough paid us a $40.0 million non-refundable, non-creditable up-front fee and assumed sole responsibility for development and commercialization of AN2690, including obtaining regulatory approvals. Schering-Plough will pay all of the remaining costs for development and commercialization of AN2690 in all indications, including paying us for our development-related transition activities, which we estimate will be performed through June 2009. Pending discussions with the FDA and the outcome of certain non-clinical testing of AN2690, we currently anticipate that Schering-Plough will initiate Phase 3 clinical trials for AN2690 in onychomycosis by the end of 2008.

        If certain development, regulatory and commercial milestones for onychomycosis are met, Schering-Plough is obligated to pay us up to $505.0 million. Schering-Plough is also obligated to pay us additional fees for each additional indication for which Schering-Plough develops AN2690 treatments if certain milestones are achieved. Schering-Plough is further obligated to pay us double-digit royalties up to twenty percent on annual net sales of AN2690 for all indications in jurisdictions where there is a valid patent claim covering the product and lesser royalties for AN2690 sales in jurisdictions where there is no valid patent claim. We retained the option to co-promote AN2690 for the treatment of onychomycosis to dermatologists in the United States, subject to certain conditions. In addition, we have the right to require Schering-Plough to purchase up to $10.0 million of our capital stock. Schering-Plough may terminate this agreement without cause at any time and we are allowed to terminate the agreement in the event that Schering-Plough materially breaches its obligations to use commercially reasonable efforts to develop and commercialize AN2690.

        In October 2007, we entered into a research and development collaboration, option and license agreement with GSK for the discovery, development, manufacture and worldwide commercialization of boron-based systemic therapeutics for at least eight product options in up to four target-based projects, one of which will target the Hepatitis C Virus (HCV) and others of which will be in the area of antibiotics. Under the agreement, we will collaborate with GSK to identify and develop boron-based small molecule product candidates.

43



        Pursuant to the agreement, GSK is obligated to pay us a $12 million non-refundable, non-creditable up-front fee in October 2007 and we have the right to require GSK to purchase $10 million of our capital stock. In each project, GSK has the option to obtain an exclusive license to develop, commercialize and market worldwide a specified number of product candidates once they have achieved proof of concept criteria. In the HCV project, GSK also has an option to obtain such an exclusive license at the time a product candidate is selected. We will be primarily responsible for the discovery and development of each product candidate from the research stage until GSK exercises an option for such product candidate, at which point GSK will assume sole responsibility for the further development and commercialization of such product candidate on a worldwide basis. GSK is obligated to make payments to us if certain development, regulatory and commercial milestones are met on a compound-by-compound basis, which range up to $252 million to $331 million in the aggregate per product candidate. GSK is further obligated to pay us double-digit tiered royalties based on sales achieved on optioned compounds. In the event that GSK exercises its option for a product candidate in the HCV project at the candidate selection stage, the discovery, development and regulatory milestone payments for which we are eligible and the product royalties payable to us would be lower. During the research term, we are committed to use reasonable efforts to discover and optimize compounds and to provide specified resources, including certain numbers of full-time equivalent scientists, on a project-by-project basis. Each party is responsible for its own research and development costs.

        We began business operations in March 2002. To date, we have not generated any revenue from product sales and have never been profitable. As of June 30, 2007, we have an accumulated deficit of $48.4 million. We have funded our operations primarily through the sale of equity securities, government contracts and grants, borrowings under debt arrangements and the up-front payment under our agreement with Schering-Plough. We expect to incur losses in future periods. The size of our future losses will depend, in part, on the rate of growth of our expenses, our ability to enter into additional licensing, research and development agreements and receipt of future payments under our agreements with Schering-Plough and GSK. Our intent is to enter into licensing and development agreements with additional partners for certain of our other product candidates and research and development programs. If this does not occur, the milestones for AN2690 in the Schering-Plough agreement are not achieved or Schering-Plough terminates our agreement, we may incur additional operating losses and our ability to expand our research and development activities and move our product candidates into later stages of development may be limited.

        Prior to 2007, we operated as a development stage company as defined in Statement of Financial Accounting Standards (SFAS) No. 7, Accounting and Reporting by Development Stage Enterprises . As a result of our progress in establishing our operations to date and the execution of and revenues from our agreement with Schering-Plough, we are no longer considered a development stage company.

        We have generated approximately $26.4 million in revenue from inception through June 30, 2007. Through 2004, we had earned $16.1 million through our contract with the U.S. Department of Defense, or DOD, for the development of antibiotics against infective anthrax. In September 2005, we were awarded a $1.0 million National Institutes of Health, or NIH, grant for the identification of targets for certain antifungal compounds, which included work on the mechanism of action of AN2690. By February 2007 we had earned and received the total amount available under the grant. In March 2007, we received a $40.0 million up-front fee that is being recognized ratably over the estimated period during which we will be performing development-related activities to transition AN2690 to Schering-Plough. The estimated period was based on the research transition plan jointly developed by Schering-Plough and us. Additionally, we are being paid for these development-related activities, which include certain preclinical and clinical projects. We estimate these activities will continue through June 2009. During the six months ended June 30, 2007, we recognized revenue of $9.3 million under the agreement, which was comprised of $5.1 million of amortization of the up-front fee and $4.2 million for development-related transition

44


activities. In the future, revenue under our agreement with Schering-Plough may also include development, regulatory and sales milestones and product royalties. In October 2007, we expect to receive a $12.0 million up-front payment under our agreement with GSK, which we expect will be recognized ratably over the research term.

        Research and development expenses consist primarily of costs associated with research activities, as well as costs associated with our product development efforts, including preclinical studies and clinical trials. Research and development expenses, including those paid to third parties, are recognized as incurred. Research and development expenses include:

        Our expenses associated with preclinical studies and clinical trials are based upon the terms of the service contracts, the amount of the services provided and the status of the related activities. We expect that research and development expenses will increase significantly in the future as we progress our product candidates through clinical development, conduct our research and development activities under our agreement with GSK, advance our discovery research projects into the preclinical stage, continue our early stage research, file for regulatory approvals, hire more employees and lease a larger facility.

        The table below sets forth our research and development expenses since January 1, 2004 for our three clinical-stage product candidates, our contract with the DOD and other programs including AN2718. A portion of our costs, including indirect costs relating to our product candidates, are not tracked on a project basis and are allocated based on management's estimate.

 
  Year Ended December 31,
  Six Months Ended June 30,
 
  2004
  2005
  2006
  2006
  2007
 
  (in thousands)

AN2690, including NIH grant expenses   $ 647   $ 5,645   $ 11,738   $ 4,282   $ 4,426
AN2728             1,364     1,181     679
AN0128     3,193     4,617     1,968     1,093     1,161
DOD contract     4,776                
Other programs, including AN2718     1,970     3,761     1,557     1,198     3,898
   
 
 
 
 
  Total research and development   $ 10,586   $ 14,023   $ 16,627   $ 7,754   $ 10,164
   
 
 
 
 

        We expect our research and development expenses to increase through the rest of 2007 and during 2008. Our October 2007 agreement with GSK requires us to commit specific resources to the collaboration activities, which will significantly increase our research and development expenditures on specific systemic drug discovery projects. However, we expect costs associated with AN2690 to decrease in the future as we transition development to Schering-Plough. We expect costs associated with AN2728 to increase as we expand the clinical activities for this program. We expect spending on AN0128 to decrease through the rest of 2007 and during 2008 due to a change in focus of the program from atopic dermatitis clinical stage

45


activities to acne and gingivitis earlier stage activities. In addition, we expect spending to increase for AN2718 and other research programs as we advance their development.

        The process of conducting preclinical studies and clinical trials necessary to obtain FDA approval is costly and time consuming. We or our partners may never succeed in achieving marketing approval for any of our product candidates. The probability of success for each product candidate may be affected by numerous factors, including preclinical data, clinical data, competition, manufacturing capability and commercial viability. Schering-Plough is solely responsible for development and commercialization of AN2690, including obtaining regulatory approvals, and therefore the progress of AN2690 is not under our control. We are responsible for development-related activities during the transition of AN2690 to Schering-Plough. In addition, under our agreement with GSK, we will be primarily responsible for the discovery and development of each product candidate from the research stage until GSK exercises an option to obtain an exclusive license to such product candidate.

        As a result of the uncertainties discussed above, the uncertainty associated with clinical trial enrollments and the risks inherent in the development process, we are unable to determine the duration and completion costs of the current or future clinical trials of our product candidates or if, or to what extent, we will generate revenues from the commercialization and sale of any of our product candidates. We anticipate that we will make determinations as to which programs to pursue and how much funding to direct to each program on an ongoing basis in response to the scientific and clinical success of each product candidate, as well as ongoing assessment as to the product candidate's commercial potential.

        Our strategy includes entering into additional collaborations with third parties for the development and commercialization of some of our product candidates. To the extent that third parties have control over preclinical development or clinical trials for some of our product candidates, then we will be dependent upon their efforts for the progress of such product candidates. We cannot forecast with any degree of certainty which of our product candidates, if any, will be subject to future collaborations or how such arrangements would affect our development plans or capital requirements.

        General and administrative expenses consist primarily of salaries and related costs for our personnel, including stock-based compensation and travel expenses, in executive, finance, business and commercial development and other administrative functions. Other general and administrative expenses include facility-related costs not otherwise included in research and development expenses, consulting costs associated with accounting and marketing research services, professional fees for legal services, including patent-related expenses, and auditing and tax services. We expect that general and administrative expenses will increase in the future as we expand our operating activities, including supporting the growth in our operations due to the GSK collaboration, move to a larger corporate facility and incur additional costs associated with being a public company.

Critical Accounting Policies and Significant Judgments and Estimates

        Our management's discussion and analysis of our financial condition and results of operations is based on our financial statements, which have been prepared in accordance with accounting principles generally accepted in the United States. The preparation of these financial statements requires us to make estimates and judgments that affect the reported amounts of assets and liabilities and the disclosure of contingent assets and liabilities at the date of the financial statements, as well as the reported revenues and expenses during the reporting periods. We base our estimates on historical experience and on various other factors that we believe to be reasonable under the circumstances and review our estimates on an ongoing basis. Actual results may differ from these estimates under different assumptions or conditions.

46



        While our significant accounting policies are described in more detail in Note 2 of our financial statements included in this prospectus, we believe the following accounting policies to be critical to the judgments and estimates used in the preparation of our financial statements.

        We recognize revenue in accordance with Securities and Exchange Commission Staff Accounting Bulletin (SAB) No. 101, Revenue Recognition in Financial Statements, as amended by SAB No. 104, Revenue Recognition and Emerging Issues Task Force (EITF) Issue No. 00-21, Revenue Arrangements with Multiple Deliverables (EITF 00-21).

        Our contract revenues are generated primarily through research and development collaboration agreements which typically include nonrefundable up-front license fees when licensing our intellectual property, the funding of research and development efforts and milestone payments. Up-front payments generally are not separable from the activity of providing research and development services because the license does not have stand-alone value separate from the research and development services provided. Accordingly, revenue from up-front payments is recognized on a straight-line basis over the contractual or estimated performance period, which is consistent with the term of the research and development obligations contained in the research and development collaboration agreement. We regularly review the basis for our estimates, and we may change the estimates if circumstances change. These changes can significantly increase or decrease the amount of revenue recognized. To date, we have not experienced significant changes in our estimates.

        Payments resulting from our research and development efforts under license agreements or government grants are recognized as the activities are performed and are presented on a gross basis in accordance with the provisions of EITF Issue No. 99-19, Reporting Revenue Gross as a Principal versus net as an Agent. Revenue is recorded gross pursuant to the criteria established by this EITF Issue because we act as a principal, with discretion to choose suppliers, bear credit risk and perform part of the services. The costs associated with these activities are reflected as a component of research and development expense in the statements of operations.

        Substantive, at-risk milestone payments will be recognized as revenue when the milestone is achieved and collectibility is assured. When payments are not for substantive and at-risk milestones revenue will be recognized on a straight-line basis over the estimated remaining term of the service period. To date, we have not received any milestone payments.

        Royalties based on reported sales of licensed products will be recognized based on contract terms when reported sales are reliably measurable and collectibility is reasonably assured.

        We estimate our preclinical study and clinical trial expenses based on the services received pursuant to contracts with research institutions and clinical research organizations that conduct these activities on our behalf. In accruing these fees, we estimate the time period over which services will be performed and the level of effort to be expended in each period. If the actual timing of the performance of services or the level of effort varies from the estimate, we will adjust the accrual accordingly. If we underestimate or overestimate the level of services performed or the costs of these services, our actual expenses could differ from our estimates. To date, we have not experienced significant changes in our estimates of preclinical study and clinical trial accruals.

        Prior to January 1, 2006, we accounted for stock-based employee compensation arrangements using the intrinsic value method in accordance with the recognition and measurement provisions of Accounting

47


Principles Board Opinion (APB) No. 25, Accounting for Stock Issued to Employees (APB 25), and related interpretations, including the Financial Accounting Standards Board Interpretation (FIN) No. 44, Accounting for Certain Transactions Involving Stock Compensation, an Interpretation of APB Opinion No. 25 as permitted by SFAS No. 123, Accounting for Stock-Based Compensation (SFAS 123). In accordance with APB 25, stock-based compensation was calculated using the intrinsic value method and represented the difference between the deemed per share market price of the stock and the per share exercise price of the stock option, if any. Any resulting stock-based compensation was deferred and amortized to expense over the grant's vesting period. For variable awards, compensation expense is measured each period as the incremental difference between the fair value of the shares and the exercise price of the stock options.

        Effective January 1, 2006, we adopted SFAS No. 123R, Share-Based Payment (SFAS 123R). SFAS 123R establishes accounting for stock-based awards exchanged for employee services. Accordingly, stock-based compensation cost is measured at the grant date, based on the fair value of the award, and is recognized as an expense over the employee's requisite service period. We elected to adopt SFAS 123R under the modified prospective method and calculate the fair value of the stock option grants using the Black-Scholes option pricing model. Under the modified prospective method, the fair values of new and previously granted but unvested stock options are recognized as compensation expense in the statement of operations over the related vesting periods, and prior period results are not restated. For options granted prior to January 1, 2006 and valued in accordance with SFAS 123, we use the graded-vested (multiple option) method for expense attribution and, prior to January 1, 2006, recognized option forfeitures as they occurred. For options granted after January 1, 2006 and valued in accordance with SFAS 123R, we use the straight-line (single option) method for expense attribution and now estimate forfeitures and only recognize expense for those shares expected to vest.

        We account for equity instruments issued to non-employees in accordance with EITF Issue No. 96-18 , Accounting for Equity Instruments That Are Issued to Other Than Employees for Acquiring, or in Conjunction with Selling Goods, or Services (EITF 96-18), which requires that these equity instruments be recorded at their fair value on the measurement date. The measurement of stock-based compensation is subject to periodic adjustment as the underlying equity instruments vest. As a result, the non-cash charge to operations for non-employee options with vesting criteria is affected each reporting period by changes in the fair value of our common stock.

        We recorded non-cash stock-based compensation expense under SFAS 123R and EITF 96-18 for employee and non-employee stock option grants of $291,000 during 2006 and $215,000 during the six months ended June 30, 2007. Based on stock options outstanding as of June 30, 2007, we had unrecognized stock-based compensation of $1.3 million, determined in accordance with SFAS 123R and EITF 96-18, of which we expect to recognize a total of approximately $333,000 and $367,000 during the remainder of 2007 and 2008, respectively. We expect to continue to grant stock options in the future, and to the extent that we do, our actual stock-based compensation expense recognized in future periods will likely increase.

        As of June 30, 2007, we had outstanding vested options to purchase 2,082,101 shares of our common stock and unvested options to purchase 2,593,902 shares of our common stock with an intrinsic value of approximately $         million and $         million, respectively, based on an assumed initial public offering price of $            per share, the midpoint of the range on the cover of this prospectus.

        The fair value of the shares of common stock that underlie the stock options we have granted has historically been determined by our board of directors, with assistance from management, based upon information available to it at the time of grant. Because, prior to this offering, there has been no public market for our common stock, our board of directors has determined the fair value of our common stock by considering a number of objective and subjective factors, including progress of research and development efforts and milestones attained in our business, sales of our convertible preferred stock to

48


arms-length investors, comparative rights and preferences of our common stock compared to the rights and preferences of our other outstanding equity securities, perspective provided by valuation analyses of our stock performed by management, the expected valuation we would obtain in an initial public offering or sale of the company and the likelihood of achieving a liquidity event given prevailing market conditions. Although it is reasonable to expect that the completion of our initial public offering will increase the value of our common stock as a result of increased liquidity and marketability and the elimination of the liquidation preference of our convertible preferred stock, the amount of additional value cannot be measured with precision or certainty.

    Common Stock Valuations

        Information on stock options granted after July 1, 2006, is summarized as follows:

Date of Issuance

  Number of
Options
Granted

  Exercise
Price

  Fair Value Estimate per Common Share
August 15, 2006   55,000   $ 0.38   $ 0.38
September 28, 2006   102,000   $ 1.66   $ 1.66
June 5, 2007   655,500   $ 2.55   $ 2.55
July 26, 2007   577,500   $ 3.00   $ 3.00
August 28, 2007   15,000   $ 3.60   $ 3.60
September 27, 2007   155,000   $ 4.25   $ 4.25
October 3, 2007   20,000   $ 4.25   $ 4.25

        We have granted stock options with exercise prices of $0.38 and $4.25 per share during the period from June 30, 2006 through October 3, 2007. We anticipate that the initial public offering price will be between $            and $            per share. The process used to estimate the fair value of our common stock and the reasons for the difference between the estimated fair value as of the date of each grant and the estimated initial public offering price are described below.

        On August 15, 2006, we granted stock options with an exercise price of $0.38 per share. The board of directors determined the fair value of our common stock on the date of grant based upon a number of the significant factors, assumptions and methodologies mentioned above and in particular our financial condition at the time. In June 2006, we had raised $5.0 million by selling shares of our Series D convertible preferred stock to existing investors and entered into a loan agreement providing for borrowings of up to $8.0 million. In the six months ended June 30, 2006, we had used net cash of $8.5 million in operations and, after giving effect to the preferred stock financing, we had cash and cash equivalents at June 30, 2006 of only $7.0 million. In July 2006, we borrowed $5.0 million under our loan agreement. As a result, by the time of our August 2006 option grants, the total of our outstanding debt and the aggregate liquidation preference of our convertible preferred stock was $42.9 million. In light of these considerations, including our cash balances, operating expense levels, debt, the liquidation preferences of the preferred stock and the uncertainty of obtaining additional funding to continue operations, the board determined that the fair value of our common stock as of August 15, 2006 was $0.38 per share. Subsequently, an in-depth retrospective valuation was performed by management that reconfirmed the fair value of our common stock to be $0.38 per share on the date of grant.

        On September 28, 2006, we granted stock options with an exercise price of $1.66 per share. In determining the fair value of our common stock, the board considered the same factors it had considered in connection with the August 2006 option grants. In particular, the board considered the fact that our financial condition had deteriorated since the August 2006 option grants as we continued to use cash in our operations. As of September 30, 2006, after giving effect to our borrowing of $5.0 million in July 2006, we had cash and cash equivalents of approximately $6.7 million. At the same time, our board had begun to consider strategic alternatives for the company. In September 2006, the board engaged a financial advisor

49



and was in active discussions both with potential acquirors and with potential partners for the development and commercialization of AN2690. By the end of September, the board was considering a number of preliminary term sheets that had been delivered by potential partners. Based on the preliminary term sheets, offset by the risk that none of these transactions would be consummated and our financial condition at the end of September 2006, the board determined that the fair value of our common stock as of September 28, 2006 was $1.66 per share.

        Although no options were granted, our board of directors directed management to perform an in-depth contemporaneous valuation as of December 31, 2006 that estimated the fair value of our common stock was $1.65 per share. We performed the valuation in accordance with applicable elements of the technical practice aid issued by the American Institute of Certified Public Accountants entitled Valuation of Privately Held Company Equity Securities Issued as Compensation . In conducting this valuation, we utilized the income approach to estimate our enterprise value and then the value of each class of equity was estimated using the option-pricing method. We applied a marketability discount of 22% to the value of our common stock to reflect the lack of liquidity for our common stock. The market comparable and market transaction methods of determining fair value were not used because it was not possible to calculate a meaningful revenue or EBIT multiple for our company. We believe the results of this valuation supports the fair value determination of the board in connection with the September 28, 2006 option grants.

        On June 5, 2007, we granted stock options with an exercise price of $2.55 per share. In determining the fair value of our common stock, the board considered a second in-depth contemporaneous valuation of our common stock performed by management as of March 31, 2007, that estimated the fair value of our common stock was $2.55 per share. This valuation was prepared using the same methodology described above, but we applied a marketability discount of 15%, which reflected the improvement in our business and the increased likelihood of a liquidity event for our stockholders since December 31, 2006. In particular, the valuation analysis took account of our improved prospects as a result of our agreement with Schering-Plough and the payment of the up-front fee of $40.0 million by Schering-Plough in March 2007. As of March 31, 2007, we had cash and cash equivalents of $40.1 million, and Schering-Plough had agreed to pay for all future costs associated with the development of AN2690. The board also considered our progress in developing AN2690 and our other product candidates since March 31, 2007, including a clinical setback in the development of AN0128 for atopic dermatitis. As a result of the setback for AN0128 and our continued use of cash since March 31, 2007, the board determined that as of June 5, 2007, the fair value of our common stock had not changed from the $2.55 per share value at March 31, 2007.

        On July 26, 2007, we granted stock options with an exercise price of $3.00 per share. In determining the fair value of our common stock, the board considered the same factors it had considered in early June 2007, as well as a third in-depth contemporaneous valuation performed by management as of June 30, 2007 that estimated the fair value of our common stock was $3.00 per share. The valuation utilized the same methodology described above, and applied a marketability discount of 10%, reflecting continuing improvement in our prospects and the increased likelihood of a liquidity event for our stockholders. As of June 30, 2007, we had cash and cash equivalents of $34.9 million, and we continued to use cash in our operations. However, in late June we had begun discussions with investment banks for purposes of considering an initial public offering of our common stock. In light of these considerations, the board determined that the fair value of our common stock as of July 26, 2007 was $3.00 per share.

        On August 28, 2007, we granted stock options with an exercise price of $3.60 per share. In determining the fair value of our common stock, the board considered the factors described above, as well as our continued use of cash in our operations. The board also considered the fact that we had selected underwriters for our initial public offering and on August 1, 2007 had held the organizational meeting for the offering. The board further considered the fact that, as of the date of grant, the filing of the registration statement for the offering was imminent, and the estimated valuation ranges for our company that were provided by the underwriters in connection with the offering. The board also considered the uncertainties

50



over whether the offering would be completed, and our anticipated cash requirements for the future. Based on these considerations, the board determined that the fair value of our common stock as of August 28, 2007 was $3.60 per share.

        On September 27, 2007 and October 3, 2007, we granted stock options with an exercise price of $4.25 per share. In determining the fair value of our common stock, the board considered the factors described above, as well as the fact that we had filed our initial registration statement on August 31, 2007, the preliminary estimated valuation ranges for our company that were provided by the underwriters in connection with the offering and the uncertainties over whether the offering would be completed. Based on these considerations, the board determined that the fair value of our common stock as of September 27, 2007 and October 3, 2007 was $4.25 per share.

        We account for our outstanding warrant under the provisions of Financial Accounting Standards Board Staff Position (FSP) No. 150-5, Issuer's Accounting under Statement No. 150 for Freestanding Warrants and Other Similar Instruments on Shares that are Redeemable (FSP 150-5), an interpretation of SFAS No. 150, Accounting for Certain Financial Instruments with Characteristics of Both Liabilities and Equity . Pursuant to FSP No. 150-5, freestanding warrants for shares that are puttable or redeemable are classified as liabilities on the balance sheet at fair value. At the end of each reporting period, changes in fair value during the period are recorded as a component of other expense. The fair value of the warrant is computed using the fair value of the convertible preferred stock and the Black-Scholes model. The fair value of the convertible preferred stock is estimated by us using valuation analyses consistent with the common stock valuation discussed above giving consideration to the preferences and other terms of the convertible preferred stock.

        We recorded the fair value of the warrant to purchase shares of our convertible preferred stock as a liability in accordance with FSP 150-5 and we will continue to adjust the liability for changes in fair value until the earlier of the exercise or expiration of the preferred stock warrant or the conversion of the warrant into a warrant to purchase common stock, at which time the liability will be reclassified to stockholders' equity (deficit).

Results of Operations

    Comparison of Six Months Ended June 30, 2006 and 2007

 
  Six Months Ended June 30,
   
 
  Increase/
(Decrease)

 
  2006
  2007
 
  (unaudited)

   
 
  (in thousands)

Revenues   $ 308   $ 9,320   $ 9,012
Research and development expenses (1)     7,754     10,164     2,410
General and administrative expenses (1)     1,656     4,143     2,487
Interest income     138     571     433
Interest expense         649     649
Other expense         301     301

(1)
Includes the following stock-based compensation

  Research and development expenses   117   176   59  
  General and administrative expenses   44   39   (5 )

        Revenues.     During the six months ended June 30, 2007, we recognized $5.1 million of the $40.0 million non-refundable, non-creditable, up-front fee received in March 2007 from Schering-Plough

51



and $4.2 million of revenue from development-related transition activities provided by us. During the six months ended June 30, 2006 and 2007, we recognized $308,000 and $51,000, respectively, of revenues for work performed under our NIH grant.

        Research and development.     The increase in research and development expenses for the first six months of 2007 compared to the same period in 2006 was primarily due to an increase of $2.7 million for our other programs and increases of $144,000 and $68,000 for the AN2690 and AN0128 programs, respectively, offset partially by a decrease of $502,000 in the AN2728 program resulting from the completion of initial preclinical studies and a clinical trial and the timing of initiation of larger clinical trials.

        General and administrative.     The increase in general and administrative expenses for the first six months of 2007 compared to the same period in 2006 was primarily due to $2.0 million for financial advisory, consulting and legal fees related to the completion of the Schering-Plough agreement, an increase of $256,000 in professional services fees to support the growth of our operations and an increase of $231,000 in personnel costs resulting from increased headcount.

        Interest income.     The increase in interest income was attributable to higher average cash balances maintained during the six months ended June 30, 2007 due to the $40.0 million up-front fee received from Schering-Plough in March 2007.

        Interest and other expense.     The increase in interest expense was primarily due to the $8.0 million borrowed in the second half of 2006. In addition, we recorded $301,000 of other expense to reflect the increase in fair value of the preferred stock warrant during the six months ended June 30, 2007.

    Comparison of Years Ended December 31, 2005 and 2006

 
  Year Ended December 31,
   
 
 
  Increase/
(Decrease)

 
 
  2005
  2006
 
 
  (in thousands)

 
Revenues   $ 107   $ 861   $ 754  
Research and development expenses (1)     14,023     16,627     2,604  
General and administrative expenses (1)     2,827     3,629     802  
Interest income     343     311     (32 )
Interest expense     44     369     325  
Other expense         136     136  

(1)
Includes the following stock-based compensation

  Research and development expenses   15   222   207
  General and administrative expenses   1   69   68

        Revenues.     In September 2005, we were awarded a $1.0 million NIH grant for research on targets for antifungal agents. The amount of revenues earned under the grant increased by $754,000 in 2006 when compared with 2005.

        Research and development.     The increase in research and development expenses in 2006 as compared to 2005 was primarily due to an increase of $6.0 million in expenses in the AN2690 development program and the incurrence of $1.4 million in expenses for the AN2728 development program. The increase was partially offset by a decrease of $2.6 million for the AN0128 development program and a decrease of $2.2 million for other programs.

52



        General and administrative.     The increase in general and administrative expenses in 2006 as compared to 2005 was primarily due to increased professional services fees and travel costs related to increased business development activities.

        Interest income.     The decrease in interest income in 2006 as compared to 2005 was due primarily to lower cash balances during 2006 than in the previous year.

        Interest and other expense.     The increase in interest expense in 2006 as compared to 2005 was primarily due to interest expense on the $8.0 million borrowed in the second half of 2006. We recorded $136,000 of other expense to reflect the increase in fair value of the preferred stock warrant during 2006.

Comparison of Years Ended December 31, 2004 and 2005

 
  Year Ended December 31,
   
 
 
  Increase/
(Decrease)

 
 
  2004
  2005
 
 
  (in thousands)

 
Revenues   $ 7,052   $ 107   $ (6,945 )
Research and development expenses (1)     10,586     14,023     3,437  
General and administrative expenses (1)     1,646     2,827     1,181  
Interest income     31     343     312  
Interest expense     42     44     2  

(1)
Includes the following stock-based compensation

  Research and development expenses     15   15
  General and administrative expenses     1   1

        Revenues.     During 2005, we recorded $107,000 of revenue related to the NIH grant, which was awarded in 2005. During 2004, we recorded $7.1 million of DOD contract revenue. This contract was terminated during 2004 by the DOD.

        Research and development.     The increase in research and development expenses in 2005 as compared to 2004 was primarily due to an increase of $5.0 million in expenses for the AN2690 program, an increase of $1.4 million in expenses for the AN0128 program and an increase of $1.8 million for other programs. These increases were offset partially by a $4.8 million decrease in expenses for the DOD program that was terminated during 2004.

        General and administrative.     The increase in general and administrative expenses in 2005 as compared to 2004 was primarily due to an increase of $535,000 for professional services fees, which was primarily related to patent-related expenses, an increase of $481,000 in personnel costs and an increase of $165,000 for other administrative expenses incurred to support our growth.

        Interest income.     The increase in interest income in 2005 as compared to 2004 was due to higher cash balances resulting from our $24.8 million Series C convertible preferred stock financing which occurred in April 2005.

        Interest expense.     Interest expense recorded during 2005 was generated from a $714,000 equipment capital lease that was outstanding from May 2003 through September 2005 plus a $3.0 million bridge loan with our existing investors that was outstanding from February 2005 to April 2005 and was converted into equity in conjunction with completion of our Series C convertible preferred stock financing. Interest expense recorded during 2004 was generated from the capital lease.

53



Income Taxes

        At December 31, 2006, we had net operating loss carryforwards for federal income tax purposes of $40.0 million and federal research and development tax credit carryforwards of $338,000. Our utilization of the net operating loss and tax credit carryforwards may be subject to annual limitations due to the ownership change limitations provided by the Internal Revenue Code and similar state provisions. The annual limitations may result in the expiration of net operating losses and credits prior to utilization. We recorded a valuation allowance to offset in full the benefit related to the deferred tax assets because realization of this benefit was uncertain.

Liquidity and Capital Resources

        Since our inception, we have financed our operations through the private placement of equity securities, government contracts and grants, debt and funding from our agreement with Schering-Plough. Through June 30, 2007, we have received aggregate net proceeds of $37.6 million from the issuance of convertible preferred stock and the issuance of convertible promissory notes that were converted into convertible preferred stock in April 2005. We also have received $17.1 million in government contract and grant revenues and borrowed $8.0 million under a loan agreement. In March 2007, we received a $40.0 million non-refundable, non-creditable up-front fee from Schering-Plough. Pursuant to our agreement with GSK, GSK is obligated to pay us a $12.0 million non-refundable, non-creditable up-front payment in October 2007. We have also earned interest on our cash and cash equivalents.

        As of June 30, 2007, we had approximately $34.9 million in cash and cash equivalents. We believe that our existing cash and cash equivalents as of June 30, 2007, along with the estimated proceeds from this offering and the concurrent private placements to Schering-Plough and GSK and interest thereon, will be sufficient to meet our anticipated cash requirements through at least December 31, 2008. However, our forecast of the period of time through which our financial resources will be adequate to support our operations is a forward-looking statement that involves risks and uncertainties, and actual results could vary materially.

        Our future capital requirements are difficult to forecast and will depend on many factors, including:

    the achievement of milestones under our agreements with Schering-Plough and GSK;

    the terms and timing of any other collaborative, licensing and other arrangements that we may establish;

    the ability to achieve research goals within our budgeted cost for the drug discovery projects that we undertake, including under our agreement with GSK;

    the initiation, progress, timing and completion of preclinical studies and clinical trials for our product candidates and potential product candidates;

    the number and characteristics of product candidates that we pursue;

    the progress, costs and results of our clinical trials;

    the outcome, timing and cost of regulatory approvals;

    delays that may be caused by changing regulatory requirements;

    the costs associated with our move to a new facility;

    the cost and timing of hiring new employees to support our continued growth;

    the costs involved in filing and prosecuting patent applications and enforcing and defending patent claims;

    the costs and timing of procuring clinical and commercial supplies of our product candidates;

54


    the costs and timing of establishing sales, marketing and distribution capabilities; and

    the extent to which we acquire or invest in businesses, products or technologies.

Contractual Obligations

        The following table summarizes our contractual obligations at June 30, 2007 and the effect such obligations are expected to have on our liquidity and cash flow in future years.

 
  Payments Due by Period
Contractual obligations

  Total
  2007 6 months
  2008 -
2010

  2011 -
2012

  Thereafter
Operating lease   $ 510   $ 170   $ 340   $   $
Notes payable (including interest)     10,205     419     9,786        
   
 
 
 
 
Total contractual obligations   $ 10,715   $ 589   $ 10,126   $   $
   
 
 
 
 

    Operating Lease

        We lease a 15,300 square-foot building consisting of office and laboratory space in Palo Alto, California, which expires in December 2008 and is cancelable on 4 months' notice.

        In October 2007, we entered into an agreement to lease a 36,960 square-foot building in Palo Alto, California consisting of office and laboratory space that we anticipate will replace our current facility as our corporate headquarters. The term of the lease is estimated to commence in April 2008 and will terminate in March 2018. Future minimum lease payments under this agreement total $14,448,000, consisting of $737,000, $1,295,000, $1,337,000 and $11,079,000 for the years ended December 31, 2008, 2009, 2010 and thereafter, respectively.

    Notes Payable

        In June 2006, we entered into a loan agreement with Lighthouse Capital Partners V, L.P. for $8.0 million, of which $5.0 million was borrowed in July 2006 and $3.0 million was borrowed in December 2006. The notes are secured by all of our assets except for our intellectual property.

        The interest rate on the notes is currently 10.25% per annum, excluding the final payment. The notes have an interest-only period through December 31, 2007, followed by 30 monthly payments of principal and interest. A $760,000 final payment is due at the end of the payment term and is being accrued over the term of the loan into interest expense.

        We enter into contracts in the normal course of business with clinical research organizations for clinical trials and clinical supply manufacturing and with vendors for preclinical research studies, research supplies and other services and products for operating purposes. These contracts generally provide for termination on notice, and therefore we believe that our noncancelable obligations under these agreements are not material.

Off-Balance Sheet Arrangements

        Since inception, we have not engaged in the use of off-balance sheet arrangements, such as structured finance, special purpose entities or variable interest entities.

Quantitative and Qualitative Disclosures about Market Risk

        The primary objective of our investment activities is to preserve our capital for the purpose of funding operations while at the same time maximizing the income we receive from our investments without significantly increasing risk. To achieve these objectives, our investment policy allows us to maintain a

55



portfolio of cash equivalents and short-term investments in a variety of high credit quality securities, including U.S. government instruments, commercial paper, money market funds and corporate debt securities. Due to the short-term nature of our investments, we believe that there is no material exposure to interest rate risk.

Recent Accounting Pronouncements

        In September 2006, the Financial Accounting Standards Board (FASB) issued SFAS No. 157, Fair Value Measurements (SFAS 157). SFAS 157 establishes a framework for measuring fair value in generally accepted accounting principles and expands disclosures about fair value measurements. SFAS 157 does not apply to the measurement of share-based payments. This Statement is effective for financial statements issued for fiscal years beginning after November 15, 2007. We have not yet determined the impact that SFAS 157 will have on our financial statements.

        In February 2007, the FASB issued SFAS No. 159, The Fair Value Option for Financial Assets and Financial Liabilities (SFAS 159). SFAS 159 permits entities to choose to measure eligible financial instruments and certain other items at fair value that are not currently required to be measured at fair value. Unrealized gains and losses on items for which the fair value option has been elected are reported in earnings at each subsequent reporting date. This Statement is effective for financial statements issued for fiscal years beginning after November 15, 2007. We have not yet determined the impact that SFAS 159 will have on our financial statements.

        In June 2007, the EITF reached a consensus on EITF Issue No. 07-03, Accounting for Nonrefundable Advance Payments for Goods or Services to Be Used in Future Research and Development Activities (EITF 07-3). Under EITF 07-03, nonrefundable advance payments for goods or services to be received in the future for use in research and development activities should be deferred and capitalized. Such amounts should be expensed as the related goods are delivered or services are performed. If our expectations change such that we do not expect the goods to be delivered or services to be rendered, the capitalized advance payment should be charged to expense. EITF 07-03 is effective for new contracts entered into beginning January 1, 2008. We have not yet determined the impact that EITF 07-03 will have on our financial statements.

56



BUSINESS

Overview

        We are a biopharmaceutical company developing novel small-molecule therapeutics derived from our boron chemistry platform. We believe that our expertise in creating new boron-based compounds enables us to develop proprietary product candidates rapidly and cost-effectively that address unmet medical needs across many therapeutic areas. We have focused initially on developing topical applications of our compounds to treat fungal, bacterial and inflammatory diseases. We believe topical therapeutics generally have lower development costs, reduced risk of side effects and faster time to market than systemic therapeutics. Our most advanced product candidate is AN2690, a novel topical antifungal in development for the treatment of toenail onychomycosis, a fungal infection of the nail and nail bed. In February 2007 we entered into a worldwide license, development and commercialization agreement with Schering-Plough for AN2690 for all indications, including the treatment of onychomycosis. Pending discussions with the FDA and the outcome of certain non-clinical testing of AN2690, we currently anticipate that Schering-Plough will initiate Phase 3 clinical trials for AN2690 in onychomycosis by the end of 2008. We also have a portfolio of other topical product candidates in development for the treatment of psoriasis, gingivitis, acne, vaginal candidiasis and tinea pedis.

        Our core technology platform is based on the use of boron to develop novel product candidates, which we believe confers a number of advantages in our drug development efforts. Boron-based compounds interact with biological targets in novel ways, and can address targets not amenable to intervention by traditional, carbon-based compounds. We have demonstrated that our boron-based compounds have antibiotic, anti-inflamatory, antiparasitic and antifungal properties, giving them broad utility across multiple disease areas. Technological advances in the synthesis of boron-based compounds have allowed us to rapidly create large families of compounds with drug-like properties. Finally, we believe the intellectual property landscape for boron-based pharmaceutical products is relatively unencumbered compared to that for carbon-based products, allowing us to build our intellectual property portfolio.

        By exploiting the advantages of our boron chemistry platform, we have discovered and advanced into clinical development several novel and proprietary boron-based product candidates that address attractive market opportunities. Our current proprietary product candidates include the following:

57


        In February 2007, we entered into an exclusive license, development and commercialization agreement with Schering-Plough for the development and worldwide commercialization of AN2690, including for the treatment of onychomycosis. Under the agreement, Schering-Plough assumed sole responsibility for development and commercialization of AN2690, including obtaining regulatory approvals. Schering-Plough will pay all of the remaining costs for development and commercialization of AN2690 in onychomycosis and other indications.

        Pursuant to the agreement, Schering-Plough paid us a $40 million non-refundable, non-creditable up-front fee and we have the right to require Schering-Plough to purchase up to $10 million of our capital stock. In addition to assuming sole responsibility for the costs of development and commercialization of AN2690, Schering-Plough is obligated to pay us up to $505 million if certain development, regulatory and commercial milestones for onychomycosis are met. Schering-Plough is also obligated to pay us additional fees for each additional indication for which Schering-Plough develops AN2690 treatments if certain milestones are achieved. Schering-Plough is further obligated to pay us double-digit royalties up to twenty percent on annual net sales of AN2690 for all indications in jurisdictions where there is a valid patent claim covering the product and lesser royalties for AN2690 sales in jurisdictions where there is no valid patent claim. We retained the option to co-promote AN2690 for the treatment of onychomycosis to dermatologists in the United States, subject to certain conditions. Schering-Plough may terminate this agreement without cause at any time.

Our Systemic Therapeutics Research Program and Collaboration with GSK

        We have developed a class of boron-based compounds that show activity in research-stage tests in treating systemic bacterial infections. One part of our strategy is to partner programs for potential systemic

58



product candidates at an early stage of development and undertake early development, preclinical and initial clinical development of resulting product candidates in conjunction with our partners.

        To that end, we entered into a research and development collaboration, option and license agreement with GSK in October 2007 for the discovery, development, manufacture and worldwide commercialization of boron-based systemic therapeutics for at least eight product options in up to four target-based projects, one of which will target HCV and others of which will be in the area of antibiotics. Under the agreement, we will collaborate with GSK to identify and develop boron-based small molecule product candidates.

        Pursuant to the agreement, GSK is obligated to pay us a $12 million non-refundable, non-creditable up-front fee in October 2007 and we have the right to require GSK to purchase $10 million of our capital stock in a private placement. In each project, GSK has the option to obtain an exclusive license to develop, commercialize and market worldwide a specified number of product candidates once they have achieved proof of concept criteria. In the HCV project, GSK also has an option to obtain such an exclusive license at the time a product candidate is selected. We will be primarily responsible for the discovery and development of each product candidate from the research stage until GSK exercises an option for such product candidate, at which point GSK will assume sole responsibility for the further development and commercialization of such product candidate on a worldwide basis. GSK is obligated to make payments to us if certain development, regulatory and commercial milestones are met on a compound-by-compound basis. Total potential payments for discovery, development, regulatory and commercial milestones range up to $252 million to $331 million per product candidate. GSK is further obligated to pay us double-digit tiered royalties on annual net sales of products containing optioned compounds in jurisdictions where there is a valid patent claim covering the product and lesser royalties for sales in jurisdictions where there is no valid patent claim. In the event that GSK exercises its option for a product candidate in the HCV project at the candidate selection stage, the discovery, development and regulatory milestone payments for which we are eligible and the product royalties payable to us would be lower.

Our Strategy

        Our objective is to discover, develop and commercialize proprietary boron-based drug compounds with superior efficacy, safety and convenience for the treatment of a variety of diseases. The key elements of our strategy to achieve this objective are to:

59


Boron Chemistry Platform

        Our core technology platform is based on the use of boron chemistry to develop novel therapies. Boron is a naturally occurring element that is ingested frequently through consumption of fruits, vegetables, milk and coffee. Boron has two attributes that we believe provide compounds with drug-like properties. First, boron-based compounds have a unique geometry that allows them to have two distinct shapes, giving boron-based drugs the ability to interact with biological targets in novel ways and to address targets not amenable to intervention by traditional, carbon-based compounds. Second, boron's reactivity allows boron-based compounds to interact with a biological target to create a change that is specific to a particular disease or condition.

        Despite the ubiquity of boron in the environment, a limited amount of research has been done to evaluate the therapeutic promise of boron-based compounds. This lack of research activity was due to the availability of carbon-based natural products and proteins as the starting points for small-molecule drug discovery. In addition, the evaluation of boron-based compounds as product candidates has been hampered by an insufficient understanding of the physical properties necessary to provide boron-based compounds with the chemical and biological attributes required of pharmaceutical therapies. Boron-based compounds have also been historically difficult to synthesize.

        Significant advances have recently been made in the science and practice of boron-based drug discovery. Advanced computational techniques have been developed to improve the understanding of boron-based compounds and their interaction with key biological targets relevant to treating human disease. Additionally, new methods and tools for the rapid synthesis of boron-based compounds have been developed to facilitate the creation of new compound families. These new compound families expand the universe of biological targets that can be addressed by small-molecule, boron-based compounds.

        We believe our focus on boron-based chemistry provides us with multiple advantages in the small-molecule drug discovery process. These advantages include:

60


Our Product Candidates

        We are currently focused on developing topical applications of our compounds to treat fungal, bacterial and inflammatory diseases. We focus our development activities on treating diseases where there is a logical match between the biological activity of our boron compounds and the unmet medical needs for a specific disease. We have three clinical programs underway for topical treatments of fungal, inflammatory and bacterial diseases in addition to preclinical programs in the same areas. We also have an active research program in the area of systemic antibiotics. The following table summarizes our current product candidates:

Product Candidate

  Therapeutic Area
  Indication
  Development Status
  Commercial Rights
AN2690   Topical antifungal   Onychomycosis   •  Completed dosing and follow-up in Phase 2 trials
  
•  Expect initiation of Phase 3 trials by the end of 2008
  Schering-Plough

AN2728

 

Topical anti-inflammatory

 

Mild to moderate psoriasis

 

•  Completed Phase 1b trial
  
•  Initiating additional Phase 1b and Phase 2 trials in 2007

 

Anacor

AN0128

 

Topical antibiotic/anti-inflammatory

 

Gingivitis and acne

 

•  Completed Phase 1b trial in acne
  
•  Evaluating next steps in development

 

Anacor

AN2718

 

Topical antifungal

 

Vaginal candidiasis and tinea pedis

 

•  Expect to file two INDs in 2008

 

Anacor

        Our most advanced product candidate is AN2690, a topical treatment for onychomycosis, which is a fungal infection of the nail and nail bed. Pending discussions with the FDA and the outcome of certain non-clinical testing of AN2690, we currently expect Schering-Plough to initiate Phase 3 clinical trials of AN2690 for onychomycosis by the end of 2008.

        Dermatophytes, fungi that infect the skin, hair or nails, are the primary cause of onychomycosis. The infection involves the nail plate, the nail bed and, in some cases, the skin surrounding the nail plate. Infection causes nails to deform, discolor, become brittle and split and the nail bed and nail plate to thicken and separate. Toenails affected by onychomycosis can become so thick that routine trimming of the nails becomes difficult and can cause pain while wearing shoes, making it difficult to walk, work or do other activities. Onychomychosis can also lead to social embarrassment, since it may be perceived to be an active infection and contagious.

61



        According to Podiatry Today , 35 to 36 million people in the United States have onychomycosis. Over 95% of such infections are onychomycosis of the toenail, according to a report in U.S. Dermatology Review . According to the manufacturer of Lamisil, 47% of those affected are not receiving treatment. For those who do seek treatment, options include debridement, oral or topical drugs or a combination of debridement and drug therapies. Debridement consists of scraping, cutting away or removal of the affected nail. If not treated, onychomycosis may persist or worsen. Because the fungi that cause onychomycosis are present in many common locations such as floors, the soil, socks and shoes, onychomycosis often recurs in susceptible individuals. Consequently, the nail can be reinfected and additional courses of treatment are frequently required even after successful treatment.

        Worldwide sales of Lamisil, the leading systemic drug for onychomycosis, peaked at $1.2 billion in 2004 and totaled $978 million in 2006. A generic version of Lamisil, terbinafine, recently became available. According to IMS Health, Penlac, the only approved topical agent for onychomycosis, reached peak annual sales in the United States of approximately $125 million in 2002 but declined to approximately $88 million in 2006, which we believe was due to its perceived lack of efficacy.

        Current therapies for onychomycosis include debridement and drug therapies. Debridement is time-consuming and only marginally effective in eliminating the fungal infection. Drug therapies are available in two types, either systemic therapies such as Lamisil, or topical products such as Penlac. According to the Lamisil product label, 38% of patients treated in clinical trials with a twelve-week course of therapy achieved 100% normal treated nail and the absence of detectable fungus. Because treatment with Lamisil can cause liver failure, patients are recommended to undergo liver function tests prior to initiating treatment. Typically those with pre-existing liver disease cannot be treated with Lamisil.

        Penlac is approved for use in conjunction with frequent debridement. In the two clinical trials cited on Penlac's product label, even with frequent debridement, only 5.5% and 8.5% of patients treated with Penlac achieved 100% clear nail growth, the absence of detectable fungus and negative fungal cultures. We believe that a significant barrier to effective treatment by topical therapies is the difficulty of formulating the drug product to penetrate the nail plate to reach the nail bed and treat the onychomycosis infection.

        By addressing the limitations of current therapies, we believe AN2690 will have a safety and efficacy profile that can make it a best-in-class therapy for the treatment of onychomycosis. In Phase 2 clinical trials, AN2690 has demonstrated efficacy in treating onychomycosis and has no observed systemic side effects.

        We have designed our topical AN2690 antifungal with three distinguishing characteristics:

62


        AN2690 has a novel mechanism of action that targets an essential protein synthesis enzyme, leucyl-transfer RNA synthetase, or LeuRS. This enzyme plays a pivotal role in fungal protein synthesis by attaching the leucine amino acid to transfer RNA, or tRNA. In addition, LeuRS also plays a key role in ensuring the correct synthesis of leucyl-transfer RNA. Our research has demonstrated that compounds that bind to the specific site on LeuRS involved in the synthesis of leucyl-transfer RNA also inhibit the attachment of leucine to tRNA, resulting in the inactivation of LeuRS and inhibiting protein synthesis within the fungal cell. The inhibition of protein synthesis leads to termination of cell growth or cell death, eliminating the fungal infection. We have shown that this inhibitory activity requires the presence of boron within the compound, as the replacement of the boron atom in AN2690 with a carbon atom inactivated the molecule. The unique boron-based mechanism of action underlying AN2690 was detailed in the June 22, 2007 issue of the journal Science .

        Resolution of onychomycosis is a two-step process. First, the fungus present in the nail plate and nail bed must be killed by treatment. Second, the fungus-free nail must return to a normal appearance by regenerating a normal nail bed and growing a new nail. Given the slow pace of nail growth, which is approximately one to two millimeters per month, twelve-month Phase 3 clinical trials are the industry standard for onychomycosis treatments to allow sufficient time for patients' nails to reach full clear nail growth.

        The FDA has established a clear clinical pathway for the evaluation of therapies to treat onychomycosis. Response to treatment of onychomycosis is measured in terms of both clinical response and mycologic response.

        Clinical response of a treated nail is defined in three categories. "Clear Nail" is considered a 100% normal nail. "Almost Clear" is considered a nail that has less than 10% abnormal nail present. "Clear Nail Growth" is the length in millimeters of new healthy nail growth observed at specified times after initiation of therapy.

        Mycologic response refers to the effect of treatments on the presence of fungi and is measured by KOH examination and fungal culture, which are separate laboratory tests. In the KOH test, material scraped from beneath the nail is examined microscopically for the presence of fungi. In the fungal culture test, the material is incubated over several weeks to determine if a fungal colony will grow. The combination of negative KOH and negative fungal culture tests is classified as a "Mycologic Cure."

        For recently approved treatments for onychomycosis, the FDA has required a composite primary endpoint at the end of a 48 to 52 week Phase 3 clinical trial consisting of a Clear Nail plus Mycologic Cure, which is considered a "Complete Cure."

        Secondary endpoints commonly used include:


        Pending discussion with the FDA and the outcome of certain non-clinical testing of AN2690, we currently anticipate that Schering-Plough will commence Phase 3 clinical trials of AN2690 by the end of 2008. We expect that the Phase 3 AN2690 clinical trials will be consistent in length of trial and endpoint with Phase 3 clinical trials of other recently approved drugs to treat onychomycosis. As such, we anticipate

63


that Schering-Plough will modify the treatment protocol for the Phase 3 clinical trials compared to our completed Phase 2 clinical trials. Trial size will be set by the need to meet the regulatory requirement for the total number of patients treated prior to approval.

        We are currently working with Schering-Plough to transition the AN2690 research and development program to them. We expect to perform certain preclinical and clinical activities for Schering-Plough in this transition. We currently estimate these activities will continue through June 2009. Schering-Plough will pay us for our development-related transition activities during this period.

        For AN2690, our three completed Phase 2 trials consisted of a six-month treatment period and six months of patient follow-up. We have one ongoing trial to demonstrate the safety and efficacy of a longer treatment period, the enrollment of which was completed in May 2007. We have also completed two pharmacokinetic studies and one dermal tolerability study of AN2690. Our Phase 2 clinical trials have enabled us to define multiple well-tolerated, efficacious doses and a dose-response relationship. We have also demonstrated that topical application to the toenails with AN2690 has led to little or no detectable systemic drug exposure in blood or urine. However, a small number of our patients who received AN2690 treatment experienced reversible skin irritation. Our Phase 2 clinical trials enabled the selection of a single concentration, or dose, of AN2690 for Phase 3 clinical trials and provided an understanding of the treatment effect associated with AN2690 that will allow the appropriate statistical calculations in the design of Phase 3 clinical trials.

        The following chart summarizes our completed Phase 2 clinical trials to date:

Number

  Type
  Dosing
  Patients
  Trial Objectives
200/200a   Double-blind   Vehicle; 2.5%; 5.0%; 7.5%   187   Demonstrate safety and efficacy compared to vehicle

201
(first and second cohorts)

 

Open-label

 

5.0%; 7.5%

 

60

 

Demonstrate safety and efficacy

203

 

Open-label

 

1.0%; 5.0%

 

60

 

Evaluate efficacy of lower doses and less frequent dosing

        In our Phase 2 clinical trials, we enrolled onychomycosis patients representative of a wide clinical spectrum of the disease and observed Clear Nail Growth and negative fungal culture across this spectrum. We believe that these results indicate that AN2690 will effectively treat patients who are representative of the population that would seek treatment for onychomycosis.

        The primary objective of Study 200/200a was to demonstrate that the efficacy of AN2690 could be differentiated from the response to a placebo not containing the product candidate, or vehicle, alone and to select the appropriate dose of AN2690 for Phase 3 clinical trials. A total of 187 patients were enrolled at multiple sites in Mexico and the United States. Certain patients were dosed with the vehicle, while other patients received the 2.5%, 5.0% or 7.5% dose. The trial was double-blind such that neither the patients nor the investigators were aware of which treatment strength or placebo was being applied. Patients dosed themselves daily for the first three months and three times per week for the remaining three months of the six-month treatment period, with an additional six months of post-treatment follow-up.

        The study was a one-year study. The study's primary endpoint was the number of patients with at least two millimeters of new Clear Nail Growth and negative fungal culture at six months. The one-year data are not yet available. At the completion of the six-month treatment phase, significantly more patients treated

64



with AN2690 (2.5%, 5.0% and 7.5%) achieved the primary endpoint, compared with the vehicle (p-value of 0.03). We believe the results are supportive of Phase 3 clinical trial initiation.

        The objective of Study 201 was to determine safety and efficacy of 5.0% and 7.5% topical solutions of AN2690 in treating onychomycosis. A total of 60 patients were enrolled at multiple sites in Mexico. Half received a 5.0% daily dose and the other half received a 7.5% daily dose for a period of six months, with all patients receiving an additional six months of follow-up assessment. The trial was open-label, such that all patients knew the treatment group to which they were assigned. The study's primary endpoints were the number of patients with at least two millimeters of new Clear Nail Growth at six months and a negative fungal culture. At the end of the six-month treatment period, 43% of patients receiving the 5.0% dose and 53% of patients receiving the 7.5% dose were observed to achieve the trial's primary endpoints.

        The objective of Study 203 was to determine safety and efficacy of lower dosing and less frequent dosing of AN2690 in treating onychomycosis. Two groups of 30 patients were enrolled at multiple sites in the United States. Half applied a 1.0% daily dose for six months and the other half applied a 5.0% daily dose for the first month, then three times per week for the remaining five months of treatment. Both treatment groups were followed for an additional six months after the end of treatment. The study's primary endpoints were the number of patients with at least two millimeters of new Clear Nail Growth at six months and a negative fungal culture. At the end of the six-month treatment period, 30% of patients receiving the 1.0% dose and 43% of patients receiving the 5.0% dose achieved the primary endpoint of at least two millimeters of new Clear Nail Growth and negative culture. We believe the results are supportive of Phase 3 clinical trial initiation.

        We have a drug development program focusing on treatment of inflammatory diseases such as psoriasis, seborrheic dermatitis, or dandruff, atopic dermatitis, or eczema, and gingivitis. AN2728 is our current product candidate in this program. We have tested AN2728 as a topical therapy for psoriasis, an inflammation of the skin caused by a reaction of the immune system, and anticipate testing it in other inflammatory skin diseases such as atopic dermatitis.

        AN2728 is designed to inhibit the release of TNF-alpha, a precursor of the inflammation associated with psoriasis and a validated target, as well as other cytokines, which are proteins involved in the inflammation process and immune responses. We believe that AN2728 has the potential to combine the effect of injectable biologics with a better safety profile than existing therapies. AN2728 has demonstrated initial safety and activity against psoriatic lesions in a Phase 1b clinical trial conducted in the first half of 2007. We plan to initiate an additional Phase 1b clinical trial and a Phase 2 efficacy clinical trial in 2007.

        Psoriasis is a chronic inflammatory skin disease that affects approximately 10 million people worldwide, according to Decision Resources . Psoriasis is characterized by thickened patches of inflamed, red skin covered with thick, silvery scales typically found at the elbows, knees, scalp and genital area. Patients can be categorized as mild, moderate or severe, with approximately 80% of patients having mild to moderate forms of the disease. The disorder ranges from a single, small, localized lesion in some patients to a severe generalized eruption. The recent introductions of new systemic biologic therapies for moderate to severe psoriasis has provided new treatment options for patients with moderate to severe disease and greatly expanded amounts spent on drugs to treat psoriasis. According to IMS Health, sales of psoriasis drugs in the United States were nearly $1 billion in 2006.

65


        There are many types of treatments for psoriasis. Most psoriasis patients use more than one treatment at any given time and may rotate treatments over time as their disease severity changes or they develop complications. Although current treatments attempt to decrease the severity of the disease, none of them cures the disease. Currently available treatments can be classified as topical, oral or injectable. According to IMS Health, 87% of all prescriptions within the United States in 2006 were for topical treatments. The most common topical treatments are topical corticosteroids, vitamin D derivatives, such as Dovonex, vitamin A derivatives, such as Tazorac, and crude coal tar preparations. The most common oral treatments are the immunosuppressive drug methotrexate and the vitamin A derivative acetretin. More recently, a number of injectable biologic drugs have entered the market such as Amevive, Enbrel, Humira, Raptiva and Remicade. The majority of these drugs are monoclonal antibodies, a type of complex protein molecule. Some of these biologics act by the inhibition of TNF-alpha. In addition to topicals, orals and injectables, psoriasis is also treated with ultraviolet light exposure. Typically, physicians initiate treatment by prescribing topical therapies to treat mild or moderate forms of psoriasis, followed by light therapy or oral treatments if the patient's disease does not improve. For patients that do not respond to oral treatments or light therapy, or who have severe psoriasis, physicians will prescribe injectable biologic treatments.

        Current topical therapies have demonstrated only moderate efficacy in decreasing disease severity and rarely achieve a complete clearing of the psoriatic lesions. Topical corticosteroids are associated with atrophy or thinning of the skin and have the potential to suppress the body's ability to make normal amounts of endogenous corticosteroids. Vitamin D analogues can cause skin irritation, and some patients report burning sensations associated with their use. Oral and injectable drugs have greater activity than topical therapies but also have well documented and significant systemic side effects such as liver toxicity, increase in blood fats and suppression of the immune system. In addition, injectable biologic drugs have potentially life threatening side effects and are very expensive, costing tens of thousands of dollars annually. Ultraviolet light treatments can be effective but require multiple visits to the doctor's office each week and have been shown to increase patients' risk of developing skin cancer.

        AN2728 is our topical product candidate for the treatment of psoriasis, which we believe has the potential to combine the effect of injectable biologics that inhibit the production of TNF-alpha and other cytokines with a better safety profile than existing therapies. We believe AN2728 has the potential to be a safe and effective therapy for the majority of psoriasis patients with mild to moderate disease as well as those patients with severe disease who utilize combination topical and systemic treatment. If approved, AN2728 would be the first topical non-steroidal treatment that inhibits TNF-alpha release.

        Inhibition of cytokines such as TNF-alpha is a well-validated approach used by injectable biologic agents such as Enbrel, Humira and Remicade to effectively treat psoriasis. AN2728, a small-molecule compound, works by inhibiting phosphodiesterase 4, or PDE4, an enzyme that is critical to the production of TNF-alpha and other cytokines, which results in the suppression and reduction of the inflammatory response associated with psoriasis. Given that AN2728 is applied topically, the potential for systemic side effects is anticipated to be relatively low compared to the systemically administered biologics.

        In the first half of 2007, we completed a Phase 1b clinical trial in Germany for AN2728 in patients with psoriasis. The study enrolled twelve patients for a twelve-day treatment. Each patient had their psoriatic lesions divided into six test areas to which one of the following was applied: AN2728 5.0% ointment, AN2728 5.0% cream, commercially-available psoriasis therapies betamethasone (Betnesol-V)

66


and tacrolimus (Protopic), vehicle cream and vehicle ointment. Evaluations of the sections were made at days one, eight and twelve. The primary endpoint of the study was the change in thickness of the psoriatic lesion as measured by sonography, and the secondary endpoint was improvement based on clinical score as evaluated by a physician. This study demonstrated that AN2728 caused a significant reduction in the thickness of psoriatic lesions compared to vehicle, at a p-value of 0.025. The mean percent reduction in infiltrate thickness for AN2728 was 54%, as compared to 48% for Protopic ointment and 72% for Betnesol-V cream. The secondary endpoint results of the clinical assessments paralleled the primary endpoint results of the sonographic assessments. No treatment-related adverse events were observed.

        We intend to begin an additional Phase 1b clinical trial and a Phase 2 clinical trial in parallel in 2007 to better characterize the safety profile of AN2728 and establish the appropriate efficacious dose for treating psoriasis. These studies will include a dose-ranging trial to assess clinical potency and a trial to assess efficacy with patient application. We are planning additional preclinical toxicity studies to assess dermal and systemic safety and tolerability. The complete Phase 2 and Phase 3 clinical development plan to confirm safety and efficacy in the intended population will involve several additional studies, which will require many more patients compared to the Phase 1b clinical trial.

        Our product candidate, AN0128, combines antibiotic properties with significant anti-inflammatory activity. We believe that this combination of antibiotic and anti-inflammatory properties gives AN0128 the potential to treat a number of indications, including gingivitis and acne.

        We are exploring opportunities with leading manufacturers of oral care products to evaluate whether to pursue development of AN0128 for gingivitis. We may also choose to develop AN0128 for the treatment of acne. The bacteria thought to cause acne is propriobacterium acnes , or P. acnes. In a Phase 1b clinical trial comparing the ability of AN0128 and a commercial product (the topical antibiotic clindamycin) to decrease the amount of P. acnes over a discrete area, fifteen patients were treated with AN0128, and the results demonstrated in vivo anti-bacterial activity of AN0128. For FDA approval of an acne product, we will need to demonstrate statistically significant efficacy in treating acne in a large patient population. We have not conducted lesion trials for AN0128. If we decide to pursue approval of AN0128 for the treatment of acne, we would need to complete Phase 2 and Phase 3 clinical trials to confirm safety and efficacy in the intended population, which would require several additional studies with significantly more patients.

        We also conducted two Phase 2 clinical trials for AN0128 for the treatment of atopic dermatitis. The results showed that AN0128 was safe but did not demonstrate statistically significant superiority to a control formulation that did not contain the product candidate, and we therefore decided not to pursue AN0128 for atopic dermatitis.

        AN0128's anti-inflammatory properties are a result of inhibition of pro-inflammatory cytokines, including TNF-alpha. In preclinical studies AN0128 has demonstrated antimicrobial activity against bacteria involved in gingivitis and shown effectiveness against bacteria in biofilms, which are generally difficult to treat. In addition, AN0128 reduced gingival inflammation in animal studies. AN0128 has also demonstrated activity in in vitro studies against antibiotic resistant strains of bacteria and other bacteria commonly found in the skin, and demonstrated inflammation-reducing activity similar to corticosteroids in animal models of inflammation.

        AN2718 is our product candidate in preclinical development for vaginal candidiasis, or yeast infections, and tinea pedis, or athlete's foot, a dermatophyte infection of the feet. AN2718 has demonstrated in preclinical studies that it has activity against fungal strains that cause infection of the skin and the yeasts associated with vaginal candidiasis, including those resistant to commonly used treatments.

67


        AN2718 appears to be well suited to target organisms that cause common skin and topical fungal infections, including trichophyton and candida fungi. The low molecular weight of AN2718 has the potential for improved bioavailability in the thick skin of the foot. Unlike the commonly used topical, Lamisil, AN2718's activity is not inhibited by keratin, which is a major component of the skin.

        AN2718 is a topical antifungal that utilizes the same mechanism as AN2690, our topical product candidate for treatment of onychomycosis. AN2690 targets an essential protein synthesis enzyme, leucyl-transfer RNA synthetase, or LeuRS. This enzyme plays a pivotal role in protein synthesis by attaching the leucine amino acid to tRNA. In addition, LeuRS also plays a key role in ensuring the correct synthesis of leucyl-transfer RNA. Our research has demonstrated for the first time that compounds that bind to the specific site on LeuRS involved in the synthesis of leucyl-transfer RNA also inhibit the attachment of leucine to tRNA, resulting in the inactivation of LeuRS and inhibiting protein synthesis within fungal or yeast cells. The inhibition of protein synthesis leads to termination of cell growth or cell death, eliminating the infection.

        Subject to the completion of preclinical studies, we intend to file separate INDs for the use of AN2718 to treat vaginal candidiasis and tinea pedis and to begin testing the topical compound in clinical trials in 2008. For vaginal candidiasis, upcoming development tasks include a Phase 1 clinical trial in normal volunteers to establish safety and tolerability upon dose escalation. Upon completion of the Phase 1 clinical trial, we intend to initiate a Phase 2a clinical trial in patients with both acute and recurrent infections. We also intend to initiate a Phase 2b clinical trial in patients with both acute and recurrent infections that will evaluate different concentrations of AN2718 compared to a positive control. For tinea pedis, the clinical development plan includes Phase 2a trials to demonstrate antifungal activity and to estimate the magnitude of the clinical response in a wide spectrum of clinical disease.

        In addition to the topical programs described above, we are conducting research to discover compounds with anti-inflammatory and anti-infective activity for topical administration.

Our Systemic Therapeutics Research Program and Collaboration with GSK

        We have developed a class of boron-based compounds that show activity in research-stage tests in treating systemic bacterial infections.

        In October 2007, we entered into a research and development collaboration, option and license agreement with GSK for the discovery, development, manufacture and worldwide commercialization of boron-based systemic therapeutics for at least eight product options in up to four target-based projects, one of which will target HCV and others of which will be in the area of antibiotics. Under the agreement, we will collaborate with GSK to identify and develop boron-based small molecule product candidates. The collaborative research term of the agreement is six years, subject to a two-year extension if agreed to by both parties.

        In each project, GSK has the option to obtain an exclusive license to develop, commercialize and market worldwide a specified number of product candidates once they have achieved proof of concept criteria, as defined in the agreement. In the HCV project, GSK also has an option to obtain such an exclusive license at the time a product candidate is selected. We will be primarily responsible for the discovery and development of each product candidate from the research stage until GSK exercises an option for such product candidate, at which point GSK will assume sole responsibility for the further development and commercialization of such product candidate on a world-wide basis, including the responsibility to obtain regulatory approvals on a country-by-country basis. During the research term, we are committed to use reasonable efforts to discover and optimize compounds pursuant to agreed research plans and to provide specified resources, including certain numbers of full-time equivalent scientists, on a

68


project-by-project basis. In addition, GSK is committed to provide specific resources, primarily to the HCV project. Each party is responsible for its own research and development costs.

        Pursuant to the agreement, GSK is obligated to pay us a $12 million non-refundable, non-creditable up-front fee in October 2007 and we have the right to require GSK to purchase $10 million of our capital stock in a private placement. In addition to assuming sole responsibility for the costs of further development and commercialization of the compounds for which it exercises an option to license, GSK is obligated to make payments to us if certain development, regulatory and commercial milestones are met on a compound-by-compound basis. Total potential payments for discovery, development, regulatory and commercial milestones range up to $252 million to $331 million per product candidate. GSK is further obligated to pay us double-digit tiered royalties on annual net sales of products containing optioned compounds in jurisdictions where there is a valid patent claim covering composition of matter or method of use of the product and lesser royalties for sales in jurisdictions where there is no such valid patent claim. In the event that GSK exercises its option for a product candidate in the HCV project at the candidate selection stage, the discovery, development and regulatory milestone payments for which we are eligible and the product royalties payable to us would be lower.

        The agreement provides for a joint research committee during the research term to oversee the research collaboration, a joint patent subcommittee responsible for coordination of intellectual property developed by the collaboration, including patent application filing and maintenance and a joint project team to oversee the HCV project. We and GSK shall appoint an equal number of members to each such committee or team and decisions shall be made on a consensus basis, except that ultimate decision-making authority with respect to the design of proof of concept trials for each research compound and determining whether proof of concept criteria have been met, is vested in GSK. GSK retains the unilateral right to terminate the agreement in its entirety upon six-months prior written notice to us and immediately with respect to any project. Should GSK exercise its unilateral right of termination with respect to the agreement or a particular project, we will have a perpetual, exclusive license to certain GSK intellectual property related to compounds under development, subject to royalty payments we would owe to GSK on commercial sales, if any, of such compounds. Either party may also terminate the agreement for cause upon failure to cure a material breach of the agreement, including each party's obligations to use commercially reasonable efforts to perform its duties under the agreement. If GSK terminates a project because of our failure to use reasonable efforts to advance the project, then GSK would obtain an exclusive license to develop and commercialize the product candidates in the project, we would not be entitled to any development or commercial milestone payments for the product candidate and our royalties on any sales of the product candidate would be reduced by 50%.

        For nine years following the effective date of the agreement, we may not research, optimize, develop or commercialize outside of the collaboration any compounds that we introduced as candidates to the project unless GSK's option to such compound terminated without being exercised or GSK later terminates an exercised option to such compound. If we choose to develop such compounds after expiration or termination of GSK's option, we may be required under certain circumstances to make certain regulatory milestone and royalty payments to GSK for such compounds.

        Upon a change of control of either party, the agreement would remain in effect. Upon a change of control of Anacor, GSK has the right to elect to exercise any remaining options to license and commercialize compounds then under development pursuant to the research collaboration. Depending upon the status of compound development and the project under which the compound is being developed, the exercise by GSK of its license options in connection with a change of control of Anacor could result in lower milestone payments and royalty rates being payable by GSK upon commercialization of such compound.

69



Our License, Development and Commercialization Agreement with Schering-Plough

        In February 2007, we entered into an exclusive license, development and commercialization agreement with Schering-Plough for the development and worldwide commercialization of AN2690, including for the treatment of onychomycosis. Under the agreement, Schering-Plough assumed sole responsibility for development and commercialization of AN2690, including obtaining regulatory approvals on a country-by-country basis until the later of ten years after the first commercial sale in a given jurisdiction or the date that any such product will no longer be subject to a valid claim of a patent or application in such jurisdiction.

        Pursuant to the agreement, Schering-Plough paid us a $40 million non-refundable, non-creditable up-front fee in March 2007, and we have the right to require Schering-Plough to purchase up to $10 million of our capital stock. Of that amount, Schering-Plough will purchase $            million from us in a private placement and the remaining $            million from certain of our existing stockholders at the initial offering price. In addition to assuming sole responsibility for the costs of development and commercialization of AN2690, Schering-Plough is obligated to make payments to us of up to $505 million if certain development, regulatory and commercial milestones for onychomycosis are met. Schering-Plough is also obligated to pay us additional fees for each additional indication for which Schering-Plough develops AN2690 treatments if certain milestones are achieved. Schering-Plough is further obligated to pay us double-digit royalties up to twenty percent on annual net sales of AN2690 for all indications in jurisdictions where there is a valid patent claim covering the product and lesser royalties for AN2690 sales in jurisdictions where there is no valid patent claim.

        We retained the option to co-promote AN2690 for the treatment of onychomycosis to dermatologists in the United States, subject to certain conditions. We may exercise our option to co-promote AN2690 to dermatologists in the United States up to 60 days following notification by Schering-Plough of its filing of an NDA with the FDA for the treatment of onychomycosis. Revenues from our co-promotion efforts will go to Schering-Plough, subject to our double-digit royalty, and Schering-Plough will reimburse us for certain of our sales expenses.

        The agreement provides for a joint steering committee during the development phase and a joint commercialization committee with respect to commercialization plans for the treatment of onychomycosis in the United States, with each committee consisting of representatives of Schering-Plough and us. Ultimate decision-making authority with respect to timing and resources devoted to development and commercialization is vested in Schering-Plough. Schering-Plough retains the right to terminate the agreement on a country-by-country basis upon 180-days prior written notice to us, provided that termination with respect to the United States will terminate the license in its entirety and termination in certain countries may terminate the license with respect to an entire region. Should Schering-Plough terminate prior to the first grant of a regulatory approval in the United States, it would be responsible to pay us all amounts necessary to complete any ongoing clinical trials up to agreed-upon limits, unless Schering-Plough's termination was due to safety concerns. We are allowed to terminate the agreement in the event that Schering-Plough materially breaches its obligations to use commercially reasonable efforts to develop and commercialize AN2690.

        Upon a change of control of either party, the agreement would remain in effect, subject to the right of Schering-Plough to terminate provisions of the agreement relating to the joint steering committee and our co-promotion rights should we be acquired by a major pharmaceutical company or a competitor in the treatment of onychomycosis.

        We are currently working with Schering-Plough to transition the AN2690 research and development program to them. We expect to continue to support Schering-Plough in this transition, which is currently estimated to occur through June 2009. Schering-Plough will pay us for our development-related transition activities during this period.

70



Sales and Marketing

        Our strategy is to develop a sales force targeting dermatologists and other specialty markets in the United States and partner with other companies for sales into other primary care markets. In addition we plan to enter into partnerships for sales outside the United States.

        Schering-Plough, which has a large primary care sales force, has the right to market AN2690 worldwide. We expect that primary care physicians will write the majority of prescriptions for AN2690 in the United States, and we expect half of overall sales will be within the United States. We granted commercialization rights to AN2690 to Schering-Plough because we expect their sales force to address this market. We also anticipate that dermatologists will write a significant number of AN2690 prescriptions, as well as the majority of prescriptions for AN2728 and AN2718, which we expect to address with our own sales force. Our agreement with Schering-Plough provides us the right to co-promote AN2690 in the United States for the treatment of onychomycosis to dermatologists, subject to certain conditions.

        We believe the reimbursement for our co-promotion efforts from Schering-Plough will enable us to build our own sales force cost-effectively and provide us with experience in commercial activities and selling pharmaceutical products to dermatologists before our other products reach the market.

        Under our agreement with GSK, upon the exercise of its option to exclusively license a product candidat