Drug Detail

Information about Zelboraf

Generic Name	Vemurafenib
IND	PLX4032
Brand Name (US)	Zelboraf
Manufacturer	Plexxicon
Drug Type	Tyrosine Kinase Inhibitor
Delivery	Oral
Approval Status	Approved for a non-GIST cancer
Indications	BRAF mutations
Overall Strategy	GIST cell based
Strategy	Block BRAF
Drug Category	BRAF inhibitor

The FDA approved Zelboraf on 17 August 2011 for the treatment of late stage metastatic melanoma. Zelboraf is a very potent inhibitor of the BRAF protein and in trials appears to be a very effecitve inhibitor of the V600E mutation in BRAF. This mutation is common in melanoma. It appears to be very selective for BRAF V600E and one of the most potent inhibitors of this protein.
A small percentage of wild-type GISTs have also been found to have the V600E BRAF mutation. It is unknown if this mutation provides the driving force in these GISTs.
Other inhibitors of Braf include:
RAF 265 (Novartis)
XL281 (Exelixis)
AZD6244 (AstraZeneca)
Sorafenib (Bayer)