Vemurafenib is an antineoplastic drug indicated for the treatment of unresectable or metastatic melanoma that is BRAF V600 mutation-positive as determined by a CFDA-approved test.
Vemurafenib is an oral small molecule inhibitor of certain mutants of BRAF serine-threonine kinase, including BRAFV600E, and it can also inhibit other kinases in vitro at effective concentrations. Certain BRAF gene mutants, including V600E, can produce constitutively activated BRAF protein, which can also cause cell proliferation in the absence of growth factors normally required for cell proliferation. Vemurafenib has anti-tumor effects in both cell models and animal models of melanoma with BRAFV600E mutation.
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