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sitravatinib malate
- Development stage
- Unknown
- Lead developer
- Bristol Myers Squibb
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Sitravatinib malate is an orally available small molecule multi-targeted receptor tyrosine kinase (RTK) inhibitor. It blocks a broad spectrum of RTKs implicated in tumor growth and progression, including Axl receptor tyrosine kinase, Eph family receptors, proto-oncogene proteins c-kit (KIT), c-mer (MERTK), c-met (MET), c-ret (RET), RON protein (MST1R), TIE-2 receptor (TEK), tropomyosin-related kinases (TRKs/NTRKs), and vascular endothelial growth factor receptors 1/2/3. Sitravatinib also inhibits PDGFR and DDR family kinases. The drug is being developed primarily for the treatment of various solid tumors such as non-small cell lung cancer (NSCLC), renal cell carcinoma, ovarian cancer, liposarcoma, soft tissue sarcoma, uveal melanoma and others. It has shown activity in preclinical models by inhibiting tumor proliferation at low nanomolar concentrations and suppressing tumor growth in vivo. Clinical trials have demonstrated manageable safety with modest clinical benefit in molecularly selected patient populations[1][5][7].
- Other names
- sitravatinib-malateSitravatinib-malate-Mirati-Therapeutics
02
Targets
AXL (AXL receptor tyrosine kinase)EPHA2 (Ephrin type-A receptor 2)EPHA3 (Ephrin Receptor A3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)RET (Rearranged during transfection receptor tyrosine kinase)MST1R (Recepteur d'origine nantais)TEK (Tie2)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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