Vemurafenib is a kinase inhibitor used to treat patients with Erdheim-Chester Disease who have the BRAF V600 mutation, and melanoma in patients who have the BRAF V600E mutation. It exerts its function by binding to the ATP-binding domain of the mutant BRAF.
- Mechanism
- Curator reviewed · 1 reference
Vemurafenib is an orally available inhibitor of mutated BRAF-serine-threonine kinase. Vemurafenif is a small molecule that interacts as a competitive inhibitor of the mutated species of BRAF. It is especially potent against the BRAF V600E mutation. Vemurafenib blocks downstream processes to inhibit tumour growth and eventually trigger apoptosis. Vemurafenib does not have antitumour effects against melanoma cell lines with the wild-type BRAF mutation.
- Primary indication
- 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.Curator reviewed · 7 structured indications
- Formula / weight
- C23H18ClF2N3O3S · 489.922 g/mol (avg)
- First approval
- Canada, 2012 · United States, 2011 · European Union, 2016
- Code names
- PLX-4032 · RG-7204 · RO-51-85426
- Brand names
Resolves to
GPXBXXGIAQBQNI-UHFFFAOYSA-NSMILESCCCS(=O)(=O)NC1=C(F)C(C(=O)C2=CNC3=NC=C(C=C23)C2=CC=C(Cl)C=C2)=C(F)C=C1What you can answer from here — as of September 12, 2026
Which drugs share a target with Vemurafenib, and which of those have an active Phase 3 trial?
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