Description
RDEA119 inhibits MEK1/2 and exhibits anticancer chemotherapeutic activity. RDEA119 is currently in clinical trials as a potential treatment for a variety of advanced cancers. This compound inhibits proliferation in thyroid cancer cells, including those containing V600E B-Raf mutations. RDEA119 also inhibits tumor growth in animal models of melanoma, colon cancer, and epidermal carcinoma.
References
Weekes CD, Von Hoff DD, Adjei AA, et al. Multicenter phase I trial of the mitogen-activated protein kinase 1/2 inhibitor BAY 86-9766 in patients with advanced cancer. Clin Cancer Res. 2013 Mar 1;19(5):1232-43. PMID: 23434733.
Liu D, Xing J, Trink B, et al. BRAF mutation-selective inhibition of thyroid cancer cells by the novel MEK inhibitor RDEA119 and genetic-potentiated synergism with the mTOR inhibitor temsirolimus. Int J Cancer. 2010 Dec 15;127(12):2965-73. PMID: 21351275.
Iverson C, Larson G, Lai C, et al. RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer. Cancer Res. 2009 Sep 1;69(17):6839-47. PMID: 19706763.