Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Melanoma

BRAF

A study in mice suggests intermittent rather than continuous dosing of Zelboraf could prevent or delay drug resistance in patients with melanoma. In xenograft mice implanted with subcutaneous melanoma tumors, intermittent dosing of the small molecule BRAF inhibitor Zelboraf did not lead to drug resistance in any animals after 200 days, whereas continuous dosing of the drug led to lethal Zelboraf resistance within 100 days. Next steps include testing the intermittent dosing regimen in patients with melanoma.
Zelboraf vemurafenib (PLX4032) is marketed by Roche and Daiichi Sankyo Co. Ltd. to treat metastatic melanoma in patients expressing the V600E BRAF mutation.
Dabrafenib (GSK2118436), a small molecule BRAF inhibitor from GlaxoSmithKline plc, is in registration to treat advanced or metastatic BRAF mutant melanoma.

SciBX 6(6); doi:10.1038/scibx.2013.136
Published online Feb. 14, 2013

Patent and licensing status undisclosed

Das Thakur, M. et al. Nature; published online Jan. 9, 2013;
doi:10.1038/nature11814
Contact: Darrin D. Stuart, Novartis Institutes for BioMedical Research, Emeryville, Calif.
e-mail:

darrin.stuart@novartis.com
Contact: Martin McMahon, University of California, San Francisco, Calif.
e-mail:

mcmahon@cc.ucsf.edu