vemurafenib

Vemurafenib is an orally administered small molecule kinase inhibitor used primarily for the treatment of unresectable or metastatic melanoma with a BRAF V600E mutation and for Erdheim-Chester disease with BRAF V600 mutations. It selectively inhibits mutated forms of the serine/threonine-protein kinase B-Raf (BRAF), particularly those harboring the V600E mutation, by binding to its ATP-binding domain. This inhibition blocks downstream signaling in the MAPK/ERK pathway, leading to reduced tumor cell proliferation and increased apoptosis in cancer cells with this mutation. The drug does not inhibit wild-type BRAF and may paradoxically stimulate tumor growth in such cases. Vemurafenib was co-developed by Roche and Plexxikon[5][7][8].

Brand names

Zelboraf

Other names

vemurafenib