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Ardea Biosciences' Lead MEK Inhibitor, RDEA119, to Enter Human Clinical Trials in Advanced Cancer Patients
Date:10/1/2007

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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 and inflammatory bowel disease, due to their ability to down-regulate inflammatory cytokines such as TNFalpha.

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 second half of 2007. Preclinical data suggest that RDEA119 may have favorable pharmaceutical properties, including the potential for convenient oral dosing and limited penetration into 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 tr
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