Ardea Biosciences Presents Data Demonstrating Favorable Pharmacokinetics And Efficacy For Mitogen-Activated ERK Kinase (MEK) Inhibitors

Main Category: Cancer / Oncology
Also Included In: Clinical Trials / Drug Trials;  Conferences;  Pharma Industry / Biotech Industry
Article Date: 16 Apr 2008 - 0:00 PDT

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Ardea Biosciences, Inc. (Nasdaq: RDEA) announced that data was presented demonstrating the potent activity and favorable pharmacokinetic profile of the Company's mitogen-activated ERK kinase (MEK) inhibitor family of compounds in the treatment of cancerous tumors.

The data were presented at the American Association for Cancer Research (AACR) annual meeting in San Diego.

The data showed that RDEA119 and RDEA436 are potent inhibitors of MEK1/2, an important step in cell cycle regulation. Both compounds suppress tumor cell growth in vitro and in vivo, have significant anti-inflammatory activity, and have limited potential for central nervous system (CNS) toxicity, a problem for other members of this class. RDEA119 is currently in Phase 1 clinical studies in advanced cancer patients and healthy volunteers for assessment of its ability to inhibit inflammatory cytokines. Preliminary Phase 1 data have demonstrated that RDEA119 has a long half-life and favorable pharmacokinetic properties, allowing for once daily oral dosing. In addition, the doses being evaluated in the Phase 1 study have achieved systemic exposure consistent with active doses in animal models of human tumors, without drug-related toxicity. Data from a human micro-dose trial, produced by Vitalea Science, Inc. using Accelerator Mass Spectrometry (AMS) technology, demonstrated that RDEA436 also has a long half-life and favorable pharmacokinetic properties.

"MEK inhibitors may have broad utility in the treatment of human cancers and inflammatory diseases. We are pleased to have two compounds in this class, both with excellent preclinical profiles and promising human pharmacokinetics, moving forward in clinical development," said Barry D. Quart, PharmD, Ardea Biosciences' President and CEO. "We constantly strive to diminish the inherent risk of drug development by having multiple compounds, from structurally different chemical classes, moving through development and we are excited to complete Phase 1 testing of our lead MEK inhibitor, RDEA119, and progress RDEA436 into Phase 1 clinical testing, in the second half of 2008."

The posters are available on the Company website (http://www.ardeabio.com) under the titles "RDEA119, a Potent and Highly Specific MEK Inhibitor is Efficacious in Mouse Tumor Xenograft Studies" and "RDEA436, a Novel MEK Inhibitor with Favorable Pharmacokinetic Properties."

About RDEA119 and RDEA436

RDEA119 and RDEA436, non-ATP competitive, highly-selective MEK inhibitors for the treatment of cancer and inflammatory diseases, are two of the compounds from Ardea's MEK inhibitor research and development program. RDEA119 has shown potential as a potent and selective inhibitor of MEK, which is believed to play an important role in cancer cell proliferation, apoptosis and metastasis. Preclinical and clinical results suggest that RDEA119 has favorable properties, including oral dosing, excellent selectivity and limited retention in the brain, which, in turn, may result in a reduced risk of central nervous system (CNS) side effects. Preclinical data shows that RDEA436 is a potent in vitro and in vivo inhibitor of MEK, has favorable pharmacokinetic properties with low CNS penetration and a long half-life in a human micro-dose study indicating the potential for once daily dosing in humans.

About Ardea Biosciences

Ardea Biosciences, of San Diego, California, is a biotechnology company focused on the discovery and development of small-molecule therapeutics for the treatment of HIV, cancer and inflammatory diseases, including gout. We have four drug candidates in clinical trials and several others in preclinical development and discovery. Our most advanced drug candidate is RDEA806, a non-nucleoside reverse transcriptase inhibitor (NNRTI), which is in a Phase 2a study for the treatment of HIV. We are also investigating RDEA806 for the treatment of gout. Our lead MEK inhibitor, RDEA119, is in Phase 1 studies in advanced cancer patients and healthy volunteers for assessment as a treatment of inflammatory diseases. RDEA436, our second generation MEK inhibitor for the treatment of cancer and inflammatory diseases, has been evaluated in human micro-dose pharmacokinetic studies and selected as a development candidate. In addition to the foregoing clinical programs, we are investigating other drug candidates in earlier stages of preclinical development and discovery.

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: sufficiency of cash resources and our goals, including the expected properties and benefits of RDEA806, RDEA119, RDEA436 and our other compounds and the results of preclinical, clinical and other studies. Risks that contribute to the uncertain nature of the forward-looking statements include: risks related to the outcome of preclinical and clinical studies, risks related to regulatory approvals, delays in commencement of preclinical and clinical studies, and costs associated with internal development and in-licensing activities. These and other risks and uncertainties are described more fully in our most recently filed SEC documents, including our Annual Report on Form 10-K and our 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. We undertake no obligation to update such statements to reflect events that occur or circumstances that exist after the date on which they were made.

Ardea Biosciences, Inc.
http://www.ardeabio.com