Zelboraf dosing rework

Novartis Institutes for BioMedical Research and University of California, San Francisco researchers have shown that simply altering the dosing regimen of Zelboraf is sufficient to prevent the development of drug resistance in mouse models of melanoma.¹ The researchers now plan to test an intermittent dosing regimen of Zelboraf in patients with melanoma.

Zelboraf vemurafenib (PLX4032) is a small molecule BRAF inhibitor marketed by Roche and Daiichi Sankyo Co. Ltd. to treat metastatic melanoma in patients expressing the V600E BRAF mutation. That mutation occurs in about 60% of melanomas and 7% of all cancers.² By inhibiting BRAF, Zelboraf blocks downstream activation of the MAPK pathway, which otherwise would trigger tumor cell proliferation...