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sitravatinib
- Development stage
- Phase 3
- Lead developer
- Bristol Myers Squibb
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Sitravatinib is an orally bioavailable, spectrum-selective small molecule inhibitor of multiple receptor tyrosine kinases (RTKs) with potential antineoplastic activity. It targets a broad range of RTKs including MET (hepatocyte growth factor receptor), TAM family receptors (TYRO3, AXL, MerTK), VEGFRs (vascular endothelial growth factor receptors 1, 2, and 3), PDGFRs (platelet-derived growth factor receptors), KIT, RET, DDR2, TRK family members, and Eph family RTKs. By inhibiting these kinases, sitravatinib disrupts signaling pathways involved in tumor cell proliferation and survival as well as the immunosuppressive tumor microenvironment. This may enhance the efficacy of immune checkpoint blockade therapies such as PD-1 inhibitors. Sitravatinib is being developed primarily for cancer indications including non-small cell lung cancer (NSCLC), renal cell carcinoma (RCC), and liposarcoma
- Other names
- sitravatinib
02
Targets
NTRK2 (Tropomyosin-related kinase receptor type B)PDGFRB (Platelet-derived growth factor receptor beta)EPHA3 (Ephrin Receptor A3)VEGFR3 (Vascular endothelial growth factor receptor 3)DDR1 (Discoidin domain receptor 1)FLT3 (Fms related receptor tyrosine kinase 3)MST1R (Recepteur d'origine nantais)KIT (c-KIT proto-oncogene receptor tyrosine kinase)RET (Rearranged during transfection receptor tyrosine kinase)AXL (AXL receptor tyrosine kinase)NTRK1 (Tropomyosin-related receptor kinase A)PDGFRA (Platelet-derived growth factor receptor alpha)VEGFR-1 (Vascular endothelial growth factor receptor 1)DDR2 (Discoidin domain receptor tyrosine kinase 2)MET (Mesenchymal-epithelial transition factor receptor)VEGFR2 (Vascular endothelial growth factor receptor 2)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)
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