MedKoo product information:

RDEA-436 

Current developer:    Ardea Biosciences, Inc.

RDEA-436 is a second-generation mitogen-activated ERK kinase inhibitor for the treatment of cancer. RDEA119 and RDEA436 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.