Vemurafenib (RG67204, PLX4032): a potent, selective BRAF kinase inhibitor.

Patrawala S, Puzanov I
Future Oncol. 2012 8 (5): 509-23

PMID: 22646766 · DOI:10.2217/fon.12.31

Vemurafenib is a potent inhibitor of the mutated BRAF kinase. Phase I and II clinical trials of vemurafenib showed response rates of more than 50% in patients with metastatic melanoma and BRAF mutation. A Phase III study comparing vemurafenib with dacarbazine in 675 previously untreated patients revealed overall survival to be 84% (95% CI: 78-89) in the vemurafenib group and 64% (95% CI: 56-73) in the dacarbazine group. Vemurafenib was associated with a relative reduction of 63% in the risk of death and 74% in the risk of either death or disease progression, as compared with dacarbazine (p < 0.001). Progression-free survival was longer in those treated with vemurafenib (median: 5.3 vs 1.6 months; hazard ratio: 0.26; 95% CI: 0.20-0.33). Response rates were 48% for vemurafenib and 5% for dacarbazine. After review of the interim analysis by an independent data and safety monitoring board, crossover from dacarbazine to vemurafenib was recommended.

MeSH Terms (9)

Antineoplastic Agents Clinical Trials as Topic Humans Indoles Melanoma Protein Kinase Inhibitors Proto-Oncogene Proteins B-raf Sulfonamides Vemurafenib

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