B-RAF inhibitors: An evolving role in the therapy of malignant melanoma

Cynthia Shepherd*, Igor Puzanov, Jeffrey A. Sosman

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

38 Scopus citations

Abstract

Immunotherapy and chemotherapy benefit few patients with metastatic melanoma, and even fewer experience durable survival benefit. These poor results come from treating melanoma as a single homogeneous disease. Recently, it has been shown that targeting activated tyrosine kinases (oncogenes) can mediate striking clinical benefits in several cancers. In 2002, a mutation at the V600E amino acid of the BRAF serine/threonine kinase was described as present in over 50% of melanomas. The mutation appeared to confer a dependency by the melanoma cancer cell on its activation of the MAP kinase pathway. The frequency and specificity of this mutation (95% at V600E of BRAF) suggests that it may be a potential target for therapy, and recent results with one inhibitor, PLX4032/RG7204, bare this out. This review updates the status of BRAF inhibitors in melanoma and what may be on the horizon.

Original languageEnglish (US)
Pages (from-to)146-152
Number of pages7
JournalCurrent oncology reports
Volume12
Issue number3
DOIs
StatePublished - 2010

Keywords

  • B-RAF inhibitors
  • Malignant melanoma

ASJC Scopus subject areas

  • Oncology

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