New Oral MEK Inhibitor, RDEA119, Shows Favorable Anti-Tumor ...( - Ardea Biosciences Inc. Presents ...)

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

SAN FRANCISCO, Oct. 24 /PRNewswire-FirstCall/ -- Ardea Biosciences, Inc. (Nasdaq: RDEA), 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
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