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New Oral MEK Inhibitor, RDEA119, Shows Favorable Anti-Tumor Properties

- Ardea Biosciences, Inc. Presents Initial Data on RDEA119 at the 2007 AACR-NCI-EORTC Conference on Molecular Targets and Cancer Therapeutics -

SAN FRANCISCO, October 24, 2007 /PRNewswire-FirstCall/ -- Ardea Biosciences, Inc. , a company focused on the discovery and development of small-molecule therapeutics for the treatment of viral diseases, cancer and inflammatory diseases, today presented preclinical data on its lead MEK inhibitor, RDEA119, at the American Association of Cancer Research (AACR), National Cancer Institute (NCI) and European Organization for Research and Treatment of Cancer (EORTC) International Conference on Molecular Targets and Cancer Therapeutics in San Francisco.

Defects in the RAS/RAF/MEK/ERK signaling pathway are closely associated with the development of human tumors, such as melanoma, colon, lung and thyroid cancers. RDEA119, the lead compound from Ardea's MEK Inhibitor Program, is a potent, non-ATP competitive, highly-selective inhibitor of mitogen-activated ERK kinase (MEK).

"Our preclinical data suggest that RDEA119 has favorable properties, including oral dosing, excellent selectivity and low central nervous system (CNS) penetration," said Barry D. Quart, PharmD, President and CEO. "In mouse xenograft studies, when RDEA119 was dosed orally once daily for 14 days, we saw significant inhibition and delay of tumor growth. We observed inhibition of pERK in tumors (the target of therapy) at significantly lower concentrations (EC50 = 73 nM), compared to those required to inhibit brain pERK (EC50 > 5,000 nM). This very limited brain penetration suggests the potential for reduced CNS side effects. We currently plan to initiate a Phase 1 study of RDEA119 in patients with advanced cancer this quarter and plan to evaluate RDEA119 for inflammatory diseases next year."

About RDEA119 and Ardea's MEK Inhibitor Program

Ardea Biosciences has a broad-based R&D program focused on the design and development of small-molecule inhibitors of mitogen-activated ERK kinase, or MEK, for the treatment of cancer and inflammatory diseases. Since defects in the RAS/RAF/MEK/ERK signaling pathway are closely associated with the development of human tumors, such as melanoma, colon, lung and thyroid cancers, inhibiting MEK signaling has promise in the treatment of many types of cancer. MEK inhibitors may also play an important role in the potential treatment of inflammatory diseases, such as rheumatoid arthritis (RA), inflammatory bowel disease (IBD) and psoriasis, due to their ability to down-regulate inflammatory cytokines, such as TNF alpha.

RDEA119, Ardea's lead compound from this program, is a potent, non-ATP competitive, highly- selective inhibitor of MEK. Ardea plans to initiate a Phase 1 clinical trial evaluating RDEA119 in advanced cancer patients in the fourth quarter of 2007. Preclinical data suggest that RDEA119 may have favorable pharmaceutical properties, including the potential for convenient oral dosing and limited retention in the brain, which, in turn, may result in a reduced risk of CNS side effects. Beyond RDEA119, the Company is evaluating a broad range of MEK inhibitors from several distinct chemical classes and plans to bring forward one of these compounds into a first-in-human study in the fourth quarter of this year.

About Ardea Biosciences, Inc.

Ardea Biosciences is focused on the discovery and development of small-molecule therapeutics for the treatment of viral diseases, cancer and inflammatory diseases. The Company plans to initiate clinical studies on four compounds this year. These include RDEA806, the Company's lead non-nucleoside reverse transcriptase inhibitor (NNRTI) for the treatment of HIV, which recently completed Phase 1 clinical trials, RDEA119, a mitogen-activated ERK kinase (MEK) inhibitor for the treatment of cancer and inflammatory diseases, which has been cleared by the FDA to enter Phase 1 clinical trials, and a follow-on NNRTI and a follow-on MEK inhibitor, both of which are scheduled to enter first-in-human studies in the fourth quarter of 2007.

Statements contained in this press release regarding matters that are not historical facts are "forward-looking statements" within the meaning of the Private Securities Litigation Reform Act of 1995. Because such statements are subject to risks and uncertainties, actual results may differ materially from those expressed or implied by such forward-looking statements. Such statements include, but are not limited to, statements regarding: Ardea's goals, including its goal of initiating a Phase 1 study of RDEA119 in patients with advanced cancer in the fourth quarter of 2007, evaluating RDEA119 for inflammatory diseases next year, and initiating clinical studies on three additional compounds this year, the expected properties and benefits of its compounds and the results of clinical and other studies. Risks that contribute to the uncertain nature of the forward-looking statements include: risks related to the outcomes of preclinical and clinical trials, risks related to regulatory approvals, delays in commencement of preclinical and clinical tests, and costs associated with internal development and in-licensing activities. These and other risks and uncertainties are described more fully in Ardea's most recently filed SEC documents, including its Annual Report on Form 10-K and Quarterly Reports on Form 10-Q, under the headings "Risk Factors." All forward-looking statements contained in this press release speak only as of the date on which they were made. Ardea undertakes no obligation to update such statements to reflect events that occur or circumstances that exist after the date on which they were made.

CONTACT: Chris Krueger, Chief Business Officer of Ardea Biosciences, Inc.,+1-760-602-9406

Web site: http://www.ardeabiosciences.com/

Ticker Symbol: (NASDAQ-NMS:RDEA)

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Posted: October 2007

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