Current Oncology Reports

, Volume 12, Issue 3, pp 146–152

B-RAF Inhibitors: An Evolving Role in the Therapy of Malignant Melanoma


    • Vanderbilt University Medical Center
  • Igor Puzanov
    • Vanderbilt University Medical Center
  • Jeffrey A. Sosman
    • Vanderbilt University Medical Center

DOI: 10.1007/s11912-010-0095-2

Cite this article as:
Shepherd, C., Puzanov, I. & Sosman, J.A. Curr Oncol Rep (2010) 12: 146. doi:10.1007/s11912-010-0095-2


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.


Malignant melanomaB-RAF inhibitors

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© Springer Science+Business Media, LLC 2010