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Vemurafenib
Pronunciation
Definition 1
A drug used to treat advanced melanoma that has a mutated (changed) form of a cell protein called BRAF. It is also being studied in the treatment of other types of cancer. Vemurafenib blocks this mutated protein, which may stop the growth of cancer cells. It is a type of kinase inhibitor and a type of targeted therapy agent. Also called BRAF (V600E) kinase inhibitor RO5185426, PLX4032, RG7204, and Zelboraf. (NCI Dictionary)
Definition 2
An orally bioavailable, ATP-competitive, small-molecule inhibitor of BRAF(V600E) kinase with potential antineoplastic activity. 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. (NCI Thesaurus)
Definition 3
A substance being studied in the treatment of cancer. BRAF (V600E) kinase is a mutated (changed) form of a cell protein called BRAF. It is found in several types of cancer, including melanoma (a type of skin cancer). Inhibiting this kinase may cause cancer cells to die. BRAF (V600E) kinase is a type of serine/threonine kinase inhibitor and a type of targeted therapy agent. (NCI Dictionary)
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