Drug intelligence / Profile preview

cabozantinib + vemurafenib

Development stage
Phase 1
Lead developer
National Cancer Institute
Modality
Small Molecules
Administration
Oral
01

Overview

Cabozantinib + vemurafenib is a combination therapy investigated for the treatment of BRAF-mutant metastatic or unresectable solid tumors and melanoma. Cabozantinib is a multi-tyrosine kinase inhibitor that targets MET, VEGFR2, and AXL, which are involved in tumor growth, angiogenesis, and resistance to BRAF inhibition. Vemurafenib is a selective inhibitor of the mutated BRAF V600E kinase, a key driver in the MAPK signaling pathway. By combining these agents, the therapy aims to achieve more robust inhibition of tumor cell proliferation and overcome MET-mediated resistance mechanisms that often limit the efficacy of BRAF inhibitor monotherapy. This combination is primarily being evaluated in clinical trials sponsored by the National Cancer Institute (NCI).

Other names
cabozantinib-s-malate + vemurafenib
02

Targets

AXL (AXL receptor tyrosine kinase)BRAF (B-Raf proto-oncogene, serine/threonine kinase)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)RET (Rearranged during transfection receptor tyrosine kinase)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)TEK (Tie2)VEGFR2 (Vascular endothelial growth factor receptor 2)

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