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 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 66 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). |
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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 | Covered Countries | Other Countries |
|---|
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