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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). |
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) 32 TYRO3 Inhibitor 8 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). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
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 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 | 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 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 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT04123704 | Phase II | Sitravatinib | Sitravatinib in Metastatic Breast Cancer | Terminated | USA | 0 |
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 |
NCT02219711 | Phase I | Sitravatinib | Phase 1/1b Study of MGCD516 in Patients With Advanced Cancer | Completed | USA | 1 |