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Pigment Cell Melanoma Res. 2010 Dec;23(6):820-7. doi: 10.1111/j.1755-148X.2010.00763.x.

PLX4032, a potent inhibitor of the B-Raf V600E oncogene, selectively inhibits V600E-positive melanomas.

Author information

1
Department of Molecular and Cellular Oncogenesis, The Wistar Institute, Philadelphia, PA, USA.

Abstract

Targeted intervention of the B-Raf V600E gene product that is prominent in melanoma has been met with modest success. Here, we characterize the pharmacological properties of PLX4032, a next-generation inhibitor with exquisite specificity against the V600E oncogene and striking anti-melanoma activity. PLX4032 induces potent cell cycle arrest, inhibits proliferation, and initiates apoptosis exclusively in V600E-positive cells in a variety of in vitro experimental systems; follow-up xenograft studies demonstrate extreme selectivity and efficacy against melanoma tumors bearing the V600E oncoproduct. The collective data support further exploration of PLX4032 as a candidate drug for patients with metastatic melanoma; accordingly, validation of PLX4032 as a therapeutic tool for patients with melanoma is now underway in advanced human (Phase III) clinical trials.

PMID:
20973932
PMCID:
PMC3623294
DOI:
10.1111/j.1755-148X.2010.00763.x
[Indexed for MEDLINE]
Free PMC Article

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