Description

Vemurafenib is a first generation selective B-Raf inhibitor that has been approved for clinical use in treating unresectable or metastatic melanoma; it exhibits anticancer chemotherapeutic activity. Vemurafenib binds the ATP-binding domain of mutant (V600E) B-Raf, present in many cancer subtypes, to inhibit downstream MEK and ERK signaling. This compound inhibits MAPK signaling and cell cycle progression in cells expressing mutant (V600E) B-Raf, but may increase MAPK signaling in cells expressing WT B-Raf. Subjects undergoing treatment with Vemurafenib have potential to develop verrucal keratosis and cutaneous squamous cell carcinoma as side effects. Vemurafenib is currently under examination as a potential treatment against tumors expressing H-Ras mutations as well.