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Therapy Name	Sitravatinib
Synonyms
Therapy Description	Sitravatinib (MGCD516) inhibits several receptor tyrosine kinases including AXL, MET, KIT, VEGFR1-3, TYRO3, RET family members, TRK family members, DDR, and Eph family members, resulting in abrogation of downstream signaling and decreased cell proliferation in tumors overexpressing the target proteins (PMID: 26675259, PMID: 30501104, PMID: 32525624).

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Drug Name	Trade Name	Synonyms	Drug Classes	Drug Description
Sitravatinib		MGCD516	AXL Inhibitor 30 DDR1 Inhibitor 10 DDR2 inhibitor 7 KIT Inhibitor 57 MERTK Inhibitor 13 MET Inhibitor 59 RET Inhibitor 53 Trk Receptor Inhibitor (Pan) 33 TYRO3 Inhibitor 7 VEGFR Inhibitor (Pan) 36	Sitravatinib (MGCD516) inhibits several receptor tyrosine kinases including AXL, MET, KIT, VEGFR1-3, TYRO3, RET family members, TRK family members, DDR, and Eph family members, resulting in abrogation of downstream signaling and decreased cell proliferation in tumors overexpressing the target proteins (PMID: 26675259, PMID: 30501104, PMID: 32525624).

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Molecular Profile	Indication/Tumor Type	Response Type	Therapy Name	Approval Status	Evidence Type	Efficacy Evidence	References
FLT3 exon 14 ins	acute myeloid leukemia	sensitive	Sitravatinib	Preclinical - Pdx & cell culture	Actionable	In a preclinical study, Sitravatinib (MGCD516) inhibited proliferation and induced cell cycle arrest in acute myeloid leukemia cells harboring a FLT3-ITD mutation in culture, increased median survival to 59 days vs 30 days in the vehicle-treated group in a cell line xenograft model, and resulted in a reduced leukemia burden in patient-derived xenograft (PDX) models compared to either Xospata (gilteritinib) or Vanflyta (quizartinib) (PMID: 36691065).	36691065
FLT3 exon 14 ins	hematologic cancer	sensitive	Sitravatinib	Preclinical - Cell line xenograft	Actionable	In a preclinical study, Sitravatinib (MGCD516) inhibited proliferation of transformed hematologic cells expressing a FLT3-ITD mutation in culture, and increased the median survival to 26 days vs 20 days in the Xospata (gilteritinib)-treated group in a cell line xenograft model (PMID: 36691065).	36691065
FLT3 exon 14 ins FLT3 D835V	hematologic cancer	resistant	Sitravatinib	Preclinical - Cell line xenograft	Actionable	In a preclinical study, transformed hematologic cells expressing a FLT3-ITD mutation with FLT3 D835V were resistant to treatment with Sitravatinib (MGCD516) in culture and in a cell line xenograft model (PMID: 36691065).	36691065
FLT3 exon 14 ins FLT3 F691L	hematologic cancer	sensitive	Sitravatinib	Preclinical - Cell line xenograft	Actionable	In a preclinical study, Sitravatinib (MGCD516) inhibited proliferation of transformed hematologic cells expressing a FLT3-ITD mutation with FLT3 F691L in culture, and increased the median survival to 26 days vs 14.5 days in the vehicle-treated group in a cell line xenograft model (PMID: 36691065).	36691065
FLT3 exon 14 ins FLT3 Y842C	hematologic cancer	sensitive	Sitravatinib	Preclinical - Cell line xenograft	Actionable	In a preclinical study, Sitravatinib (MGCD516) inhibited proliferation of transformed hematologic cells expressing FLT3-ITD with FLT3 Y842C in culture, and resulted in an increased median survival compared to the vehicle-treated group (P<0.001) in a cell line xenograft model (PMID: 36691065).	36691065
FLT3 exon 14 ins FLT3 D835F	hematologic cancer	resistant	Sitravatinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed hematologic cells expressing a FLT3-ITD mutation with FLT3 D835F were resistant to treatment with Sitravatinib (MGCD516) in culture (PMID: 36691065).	36691065
FLT3 exon 14 ins FLT3 D835Y	hematologic cancer	resistant	Sitravatinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed hematologic cells expressing FLT3-ITD mutation with FLT3 D835Y were resistant to treatment with Sitravatinib (MGCD516) in culture (PMID: 36691065).	36691065

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Clinical Trial	Phase	Therapies	Title	Recruitment Status	Covered Countries	Other Countries
NCT04887870	Phase II	Ipilimumab + Sitravatinib Nivolumab + Sitravatinib Enfortumab vedotin-ejfv + Sitravatinib Pembrolizumab + Sitravatinib Sitravatinib	Study of Sitravatinib With or Without Other Anticancer Therapies Receiving Clinical Benefit From Parent Study	Active, not recruiting	USA	0
NCT02219711	Phase I	Sitravatinib	Phase 1/1b Study of MGCD516 in Patients With Advanced Cancer	Completed	USA	1
NCT02978859	Phase II	Sitravatinib	MGCD516 in Advanced Liposarcoma and Other Soft Tissue Sarcomas	Completed	USA	0
NCT04123704	Phase II	Sitravatinib	Sitravatinib in Metastatic Breast Cancer	Terminated	USA	0

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