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Vemurafenib (also known as PLX4032, RG7204 or RO5185426, marketed as Zelboraf) is an orally bioavailable, ATP-competitive, small-molecule inhibitor of BRAF(V600E) kinase with potential antineoplastic activity. Vemurafenib received FDA approval for the treatment of late-stage melanoma on August 17, 2011. Vemurafenib selectively binds to the ATP-binding site of BRAF(V600E) kinase and inhibits its activity, which may result in an inhibition of an over-activated MAPK signaling pathway downstream in BRAF(V600E) kinase-expressing tumor cells and a reduction in tumor cell proliferation. Approximately 90% of BRAF gene mutations involve a valine-to-glutamic acid mutation at residue 600 (V600E); the oncogene protein product, BRAF(V600E) kinase, exhibits a markedly elevated activity that over-activates the MAPK signaling pathway. The BRAF(V600E) gene mutation has been found to occur in approximately 60% of melanomas, and in about 8% of all solid tumors, including melanoma, colorectal, thyroid and other cancers. Vemurafenib received FDA approval for the treatment of late-stage melanoma on August 17, 2011.
1. Nature advance online publication 7 September 2010 | doi:10.1038/nature09454; Received 19 May 2010; Accepted 31 August 2010; Published online 7 September 2010
Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma