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|Therapy Name||Entospletinib + Midostaurin|
|Drug Name||Trade Name||Synonyms||Drug Classes||Drug Description|
|Entospletinib||GS-9973|GS 9973|GS9973||SYK Inhibitor 15||Entospletinib (GS-9973) is a selective spleen tyrosine kinase (Syk) inhibitor, which in turn inhibits B-cell receptor signaling, leading to suppression of cell migration and inhibition of survival (PMID: 24779514, PMID: 32156743).|
|Midostaurin||Rydapt||PKC412|CGP 41251||CSF1R Inhibitor 28 FLT3 Inhibitor 64 KIT Inhibitor 57 PKC alpha Inhibitor 6 PKC beta Inhibitor 6 PKC Inhibitor (Pan) 11 VEGFR2 Inhibitor 37||Rydapt (midostaurin) is a multi-kinase inhibitor with activity against FLT3, KIT, PDGFRB, KDR (VEGFR2) and PKC, with higher selectivity for conventional PKC isoforms, which induces cell cycle arrest and apoptosis (PMID: 12124173, PMID: 23127174, PMID: 15914319). Rydapt (midostaurin) is FDA approved for FLT3-mutant AML in combination with chemotherapy, and is approved for use in aggressive systemic mastocytosis, systemic mastocytosis with associated hematological neoplasm, or mast cell leukemia as a single therapy (FDA.gov).|
|Molecular Profile||Indication/Tumor Type||Response Type||Therapy Name||Approval Status||Evidence Type||Efficacy Evidence||References|
|CBL Q365_E366insSK FLT3 pos||hematologic cancer||sensitive||Entospletinib + Midostaurin||Preclinical - Cell culture||Actionable||In a preclinical study, the addition of Entospletinib to treatment with Rydapt (midostaurin) resulted in enhanced inhibition of proliferation of cells expressing wild-type FLT3 and CBL Q365_E366insSK in culture (PMID: 31943762).||31943762|
|Clinical Trial||Phase||Therapies||Title||Recruitment Status||Covered Countries||Other Countries|