Drug intelligence / Profile preview

cabozantinib + gefitinib

Development stage
Preclinical
Lead developer
Exelixis
Modality
Small Molecules
Administration
Oral
01

Overview

A combination therapy consisting of cabozantinib and gefitinib. Cabozantinib is a multi-target tyrosine kinase inhibitor that targets VEGFR-1, -2, -3, KIT, TRKB, FLT-3, AXL, RET, MET, and TIE-2, while gefitinib is an EGFR tyrosine kinase inhibitor. This combination has shown synergistic effects in preclinical studies, particularly in crizotinib-resistant non-small cell lung cancer models with ROS1 fusion.

02

Targets

AXL (AXL receptor tyrosine kinase)EGFR (Epidermal growth factor receptor)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)TEK (Tie2)NTRK2 (Tropomyosin-related kinase receptor type B)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)

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