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Updated: May 17, 2026

Characterize Disease-related Mutants of RAF Family Kinases by Using a Set of Practical and Feasible Methods
07:49

Characterize Disease-related Mutants of RAF Family Kinases by Using a Set of Practical and Feasible Methods

Published on: July 17, 2019

Vemurafenib: the first drug approved for BRAF-mutant cancer

Gideon Bollag1, James Tsai, Jiazhong Zhang

  • 1Plexxikon, 91 Bolivar Drive, Berkeley, California 94710, USA. gbollag@plexxikon.com

Nature Reviews. Drug Discovery
|October 13, 2012
PubMed

Insights

Targeting the BRAF oncogene with vemurafenib has transformed melanoma treatment. This review covers BRAF biology, vemurafenib discovery, and its clinical journey for BRAF-mutated cancers.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Driver oncogenes, such as BRAF, are critical targets in cancer therapy.
  • The BRAF oncogene is implicated in approximately 50% of melanomas and other cancers.
  • Oncogenic BRAF's role as a druggable kinase makes it a key focus for small-molecule drug development.

Purpose of the Study:

  • To review the biology of the BRAF oncogene.
  • To describe the identification and development of vemurafenib, a targeted therapy for BRAF-mutated cancers.
  • To outline the clinical milestones and future directions for BRAF-targeted therapies.

Main Methods:

  • Review of scientific literature on BRAF oncogene and vemurafenib.
  • Analysis of vemurafenib's clinical development pathway and regulatory approvals.
  • Examination of technological advancements in identifying and targeting oncogenic drivers.

Main Results:

  • Vemurafenib (Zelboraf) was approved for BRAF-mutated metastatic melanoma in the US (2011) and EU (2012).
  • The development of vemurafenib highlights the success of targeting specific oncogenic drivers.
  • BRAF-targeted therapy represents a significant advancement in personalized cancer treatment.

Conclusions:

  • Targeting the BRAF oncogene has revolutionized melanoma treatment.
  • Vemurafenib's development provides a model for precision medicine in oncology.
  • Continued research into BRAF biology and drug development holds promise for future cancer therapies.

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