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Drug intelligence / Profile preview
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
AXL (AXL receptor tyrosine kinase)DDR1 (Discoidin domain receptor 1)DDR2 (Discoidin domain receptor tyrosine kinase 2)EPHA3 (Ephrin Receptor A3)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)NTRK1 (Tropomyosin-related receptor kinase A)NTRK2 (Tropomyosin-related kinase receptor type B)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)RET (Rearranged during transfection receptor tyrosine kinase)MST1R (Recepteur d'origine nantais)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)SRC (Proto-oncogene tyrosine-protein kinase Src)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)EPH (EPH receptor family)MERTK (MER proto-oncogene, tyrosine kinase)Trk (Trk receptor family)
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