BRAF inhibitors: the current and the future

Curr Opin Pharmacol. 2015 Aug;23:68-73. doi: 10.1016/j.coph.2015.05.015. Epub 2015 Jun 10.

Abstract

The introduction of BRAF inhibitors (BRAFi), vemurafenib and dabrafenib, revolutionized BRAFV600-mutated metastatic melanoma treatment with improved response rate and overall survival compared to standard chemotherapy. However, the mechanism related cutaneous toxicity remains a concern. In addition, intrinsic and acquired resistance remain the key challenges in BRAFi therapy. Extensive efforts to elucidate the mechanisms have led to an improved understanding of disease biology and resulted in exploration of multiple new therapeutic options. While the future looks bright with multiple new therapeutic strategies in exploration and possible new generations of BRAFi, there are questions remaining to be answered to enable more efficient use of BRAFi in cancer therapy.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage*
  • Drug Resistance, Neoplasm / drug effects
  • Forecasting
  • Humans
  • Imidazoles / administration & dosage
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Oximes / administration & dosage
  • Protein Kinase Inhibitors / administration & dosage*
  • Proto-Oncogene Proteins B-raf / antagonists & inhibitors*
  • Proto-Oncogene Proteins B-raf / metabolism

Substances

  • Antineoplastic Agents
  • Imidazoles
  • Oximes
  • Protein Kinase Inhibitors
  • BRAF protein, human
  • Proto-Oncogene Proteins B-raf
  • dabrafenib