Therapy Detail

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Therapy Name Entospletinib + Midostaurin
Synonyms
Therapy Description

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Entospletinib GS-9973|GS 9973|GS9973 SYK Inhibitor 14 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 24 FLT3 Inhibitor 55 KIT Inhibitor 51 PKC alpha Inhibitor 6 PKC beta Inhibitor 6 PKC Inhibitor (Pan) 10 VEGFR2 Inhibitor 35 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).

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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

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Clinical Trial Phase Therapies Title Recruitment Status


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