Analysis of two Phase 1 healthy volunteer studies of the Company's lead NNRTI candidate, RDEA806, revealed statistically significant reduction of serum uric acid (sUA) compared to placebo. In order to further understand the mechanism responsible for the sUA lowering effect, extensive experiments were conducted. Based on these studies, RDEA594 was identified as a major metabolite of RDEA806 in both humans and animals. RDEA594 exhibits a concentration-dependent inhibitory effect on the URAT1-mediated uptake of uric acid ex vivo and increases uric acid excretion in animal models. These findings suggest that RDEA594's effect on both the uptake and excretion of uric acid is responsible for essentially all of the uric acid lowering effects seen with its prodrug, RDEA806.
RDEA119, a non-ATP competitive, highly-selective MEK inhibitor for the
treatment of inflammatory diseases and cancer, is the Company's lead
compound from its MEK inhibitor research and development program. RDEA119
has shown potential as a potent inhibitor of MEK, which is believed to play
an important role in inflammation, as well as 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. The Company
is also investigating a second generation MEK inhibitor, RDEA436, for
potential use in inflammatory dise
|SOURCE Ardea Biosciences, Inc.|
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