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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
NTRK2 (Tropomyosin-related kinase receptor type B)AXL (AXL receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)TEK (Tie2)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)EGFR T790M (Epidermal growth factor receptor T790M mutant)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)
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