Therapy Detail

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Therapy Name Entospletinib
Synonyms
Therapy Description

Entospletinib 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).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Entospletinib GS-9973|GS 9973|GS9973 SYK Inhibitor 13 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).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
DNMT3A mut NPM1 mut acute myeloid leukemia predicted - sensitive Entospletinib Preclinical - Patient cell culture Actionable In a preclinical study, co-occurrence of DNMT3A and NPM1 mutations correlated with sensitivity to Entospletinib in patient-derived acute myeloid leukemia samples in an ex vivo assay (PMID: 30333627). 30333627
FLT3 exon 14 ins NPM1 mut acute myeloid leukemia predicted - sensitive Entospletinib Preclinical - Patient cell culture Actionable In a preclinical study, co-occurrence of FLT3-ITD and NPM1 mutations correlated with sensitivity to Entospletinib in patient-derived acute myeloid leukemia samples in an ex vivo assay (PMID: 30333627). 30333627
FLT3 exon 14 ins acute myeloid leukemia predicted - sensitive Entospletinib Preclinical - Patient cell culture Actionable In a preclinical study, FLT3-ITD mutations correlated with sensitivity to Entospletinib in patient-derived acute myeloid leukemia samples in an ex vivo assay (PMID: 30333627). 30333627
Unknown unknown chronic lymphocytic leukemia not applicable Entospletinib Phase II Actionable In a Phase II clinical trial, treatment with entospletinib resulted in a progression-free survival (PFS) rate of 70.1% at 24 weeks, with a median PFS of 13.8 months, and a objective response rate of 61% (24/41; all partial responses) in patients with chronic lymphocytic leukemia (PMID: 25696919). 25696919
NPM1 mutant acute myeloid leukemia predicted - sensitive Entospletinib Preclinical - Patient cell culture Actionable In a preclinical study, NPM1 mutations correlated with sensitivity to Entospletinib in patient-derived acute myeloid leukemia samples in an ex vivo assay (PMID: 30333627). 30333627
DNMT3A mut FLT3 exon 14 ins NPM1 mut acute myeloid leukemia predicted - sensitive Entospletinib Preclinical - Patient cell culture Actionable In a preclinical study, co-occurrence of FLT3-ITD, DNMT3A, and NPM1 mutations correlated with sensitivity to Entospletinib in patient-derived acute myeloid leukemia samples in an ex vivo assay (PMID: 30333627). 30333627

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Clinical Trial Phase Therapies Title Recruitment Status
NCT01799889 Phase II Entospletinib A Phase 2 of Entospletinib in Subjects With Relapsed or Refractory Hematologic Malignancies Completed
NCT02343939 Phase Ib/II Decitabine Cytarabine + Daunorubicin Entospletinib Entospletinib Monotherapy and in Combination With Chemotherapy in Adults With Acute Myeloid Leukemia (AML) Terminated


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