Format

Send to

Choose Destination
Curr Oncol Rep. 2010 May;12(3):146-52. doi: 10.1007/s11912-010-0095-2.

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

Author information

1
Vanderbilt University Medical Center, 1211 Medical Center Drive, Nashville, TN 37232, USA. cynthia.shepherd@vanderbilt.edu

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.

PMID:
20425073
DOI:
10.1007/s11912-010-0095-2
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Springer
Loading ...
Support Center