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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 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 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
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 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 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 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 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

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT04123704 Phase II Sitravatinib Sitravatinib in Metastatic Breast Cancer Terminated USA 0
NCT02219711 Phase I Sitravatinib Phase 1/1b Study of MGCD516 in Patients With Advanced Cancer Completed USA 1
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
NCT02978859 Phase II Sitravatinib MGCD516 in Advanced Liposarcoma and Other Soft Tissue Sarcomas Completed USA 0


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