Vemurafenib for the treatment of BRAF mutant metastatic melanoma.
Vemurafenib was the first selective BRAF inhibitor licensed in cancer. It is indicated for the treatment of patients affected by advanced melanoma with BRAF V600 mutation. It has shown successful results in terms of efficacy together with a favorable toxicity profile. Other compounds such as the BRAF inhibitor dabrafenib and the immunotherapeutic agent ipilimumab are also approved in the same group of patients. This article reviews the chemistry, pharmacokinetics, pharmacodynamics and clinical development of vemurafenib. Moreover, its efficacy and toxicity are compared with dabrafenib and ipilimumab. A number of trials with vemurafenib alone or in combination with other drugs are also analyzed. These trials will determine the role of vemurafenib in the treatment of BRAF mutant melanoma in forthcoming years.
['Martin-Liberal|Juan|J|', 'Larkin|James|J|']
D000911:Antibodies, Monoclonal D000970:Antineoplastic Agents D000971:Antineoplastic Combined Chemotherapy Protocols D002986:Clinical Trials as Topic D006801:Humans D007093:Imidazoles D007167:Immunotherapy D007211:Indoles D008545:Melanoma D009154:Mutation D009362:Neoplasm Metastasis D010091:Oximes D047428:Protein Kinase Inhibitors D048493:Proto-Oncogene Proteins B-raf D013449:Sulfonamides D016896:Treatment Outcome D000077484:Vemurafenib
vemurafenib BRAF melanoma dabrafenib ipilimumab chemistry pharmacokinetics pharmacodynamics MAPK MEK