Therapy Detail

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Therapy Name Dubermatinib
Synonyms
Therapy Description

Dubermatinib (TP-0903) is a selective Axl inhibitor that inhibits tumor cell survival (PMID: 22247788, PMID: 32460059, PMID: 31992541).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Dubermatinib TP-0903 AXL Inhibitor 30 Dubermatinib (TP-0903) is a selective Axl inhibitor that inhibits tumor cell survival (PMID: 22247788, PMID: 32460059, PMID: 31992541).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FLT3 exon 14 ins hematologic cancer sensitive Dubermatinib Preclinical - Cell culture Actionable In a preclinical study, Dubermatinib (TP-0903) inhibited growth of transformed cells expressing a FLT3-ITD mutation in culture (PMID: 33268594). 33268594
FLT3 exon 14 ins FLT3 D835Y hematologic cancer sensitive Dubermatinib Preclinical - Cell culture Actionable In a preclinical study, Dubermatinib (TP-0903) inhibited growth of transformed cells expressing a FLT3-ITD mutation and FLT3 D835Y in culture (PMID: 33268594). 33268594
FLT3 exon 14 ins NRAS G12D acute myeloid leukemia predicted - sensitive Dubermatinib Preclinical - Cell culture Actionable In a preclinical study, Dubermatinib (TP-0903) inhibited growth of acute myeloid leukemia cells harboring a FLT3-ITD mutation and NRAS G12D in culture (PMID: 33268594). 33268594
FLT3 D835H hematologic cancer sensitive Dubermatinib Preclinical - Cell culture Actionable In a preclinical study, Dubermatinib (TP-0903) inhibited growth of transformed cells expressing FLT3 D835H in culture (PMID: 33268594). 33268594
FLT3 exon 14 ins acute myeloid leukemia sensitive Dubermatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Dubermatinib (TP-0903) treatment resulted in cell cycle arrest and apoptosis, induced differentiation, and inhibited growth of acute myeloid leukemia cell lines harboring a FLT3-ITD mutation in culture, and reduced tumor growth and increased survival in cell line xenograft models (PMID: 33268594). 33268594
FLT3 exon 14 ins FLT3 D835Y acute myeloid leukemia sensitive Dubermatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Dubermatinib (TP-0903) treatment resulted in cell cycle arrest and apoptosis, induced differentiation, and inhibited growth of acute myeloid leukemia cells harboring a FLT3-ITD mutation and FLT3 D835Y in culture, and reduced tumor growth and increased survival in cell line xenograft models (PMID: 33268594). 33268594
FLT3 exon 14 ins FLT3 F691L hematologic cancer sensitive Dubermatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Dubermatinib (TP-0903) treatment decreased phosphorylation of Flt3 and Stat5 and inhibited growth of transformed cells expressing a FLT3-ITD mutation and FLT3 F691L in culture, and reduced peripheral blood tumor burden in cell line xenograft models (PMID: 33268594). 33268594
FLT3 exon 14 ins FLT3 D835H hematologic cancer sensitive Dubermatinib Preclinical - Cell culture Actionable In a preclinical study, Dubermatinib (TP-0903) inhibited growth of transformed cells expressing a FLT3-ITD mutation and FLT3 D835H in culture (PMID: 33268594). 33268594
FLT3 exon 14 ins IDH2 R140Q acute myeloid leukemia predicted - sensitive Dubermatinib Preclinical Actionable In a preclinical study, Dubermatinib (TP-0903) treatment inhibited growth and colony formation of cells isolated from a transgenic mouse model of acute myeloid leukemia harboring a FLT3-ITD mutation and IDH2 R140Q in culture, and increased survival in mouse models (PMID: 33268594). 33268594
AXL pos TYRO3 over exp chronic lymphocytic leukemia sensitive Dubermatinib Preclinical Actionable In a preclinical study, Dubermatinib (TP-0903) inhibited survival and induced apoptosis in Axl-positive and Tyro3-over expressing B-cells derived from chronic lymphocytic leukemia patients (PMID: 25673699). 25673699
FLT3 D835Y hematologic cancer sensitive Dubermatinib Preclinical - Cell culture Actionable In a preclinical study, Dubermatinib (TP-0903) inhibited growth of transformed cells expressing FLT3 D835Y in culture (PMID: 33268594). 33268594

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT02729298 Phase I Dubermatinib First-in-human Study of Oral TP-0903 (a Novel Inhibitor of AXL Kinase) in Patients With Advanced Solid Tumors Completed USA 0
NCT03572634 Phase Ib/II Dubermatinib Dubermatinib + Ibrutinib Phase 1/2 Study of TP-0903 (an Inhibitor of AXL Kinase) in Patients With Previously Treated CLL Terminated USA 0
NCT04518345 Phase Ib/II Dubermatinib Azacitidine + Dubermatinib TP-0903 for the Treatment of FLT3 Mutated Acute Myeloid Leukemia Completed USA 0


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