Vemurafenib is a competitive kinase inhibitor with activity against BRAF kinase with mutations like V600E. It exerts its function by binding to the ATP-binding domain of the mutant BRAF. Vemurafenib was co-developed by Roche and Plexxikon and it obtained its FDA approval on August 17, 2011, under the company Hoffmann La Roche. After approval, Roche in collaboration with Genentech launched a broad development program.
Vemurafenib is approved since 2011 for the treatment of metastatic melanoma with a mutation on BRAF in the valine located in the exon 15 at codon 600, this mutation is denominated as V600E. The V600E mutation, a substitution of glutamic acid for valine, accounts for 54% of the cases of cutaneous melanoma.
Vemurafenib approval was extended in 2017, for its use as a treatment of adult patients with Erdheim-Chester Disease whose cancer cells present BRAF V600 mutation. Erdheim-Chester disease is an extremely rare histiocyte cell disorder that affects large bones, large vessels, central nervous system, as well as, skin and lungs. It is reported an association of Erdheim-Chester disease and V600E mutation.
Centre Georges François Leclerc, Dijon, France
Memorial Sloan-Kettering Cancer Center, New York, New York, United States
Arizona Oncology, Tucson, Arizona, United States
Beth Israel Deaconess Medical Center (BIDMC), Boston, Massachusetts, United States
The Angeles Clinic, Los Angeles, California, United States
Georgetown Lombardi Comprehensive Cancer Center, Washington, D.C., District of Columbia, United States
Memorial Sloan Kettering Cancer Center, New York, New York, United States
University Of California Los Angeles, Los Angeles, California, United States
Memorial Sloan-Kettering Cancer Center, New York, New York, United States
Dana Farber Cancer Inst, Boston, Massachusetts, United States
University "Mother Theresa" Hospital Center; Oncology Department, Tirana, Albania
Hospital Britanico; Oncologia, Buenos Aires, Argentina
Fundación CIDEA, Buenos Aires, Argentina
The Angeles Clinic and Research Institute, Santa Monica Office, Santa Monica, California, United States
UCLA Department of Medicine, Los Angeles, California, United States
University of California at San Francisco, San Francisco, California, United States
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