Drug intelligence / Profile preview

vemurafenib + sorafenib

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

Vemurafenib + sorafenib is an experimental combination therapy consisting of two orally available, small molecule kinase inhibitors, vemurafenib and sorafenib. **Vemurafenib** is a selective BRAF kinase inhibitor, particularly effective against tumors with the BRAF V600E mutation, and is approved for the treatment of metastatic melanoma and Erdheim–Chester disease with BRAF mutations. **Sorafenib** is a multikinase inhibitor with activity against BRAF, RAF1 (CRAF), vascular endothelial growth factor receptors (VEGFR-1, -2, -3), and platelet-derived growth factor receptor (PDGFR), and is approved for advanced hepatocellular, renal, and differentiated thyroid carcinomas. The rationale for combination therapy is to overcome resistance to BRAF inhibition (typically vemurafenib) that arises through compensatory activation of alternative pathways, primarily RAF/RAS signaling. Preclinical and early clinical studies suggest that combined BRAF/MEK and multikinase inhibition with vemurafenib and sorafenib leads to enhanced cell death, decreased tumor proliferation, and possibly improved responses in patients who have developed resistance to BRAF inhibitors, especially in melanoma and other BRAF-mutant cancers[1][2][6].

Brand names
Zelboraf + Nexavar
Other names
vemurafenib + sorafenib
02

Targets

ARAF (Proto-oncogene serine/threonine-protein kinase A-Raf)VEGFR2 (Vascular endothelial growth factor receptor 2)RAF1 (c-Raf-1 (Y340D/Y341D))RIPK1 (Receptor-interacting serine/threonine-protein kinase 1)PDGFRB (Platelet-derived growth factor receptor beta)BRAF V600E

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