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 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). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| 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 |
| 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 |
| 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 |
| 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 |
| FLT3 exon 14 ins | acute myeloid leukemia | sensitive | Entospletinib | Preclinical - Cell culture | Actionable | In a preclinical study, Entospletinib (GS-9973) treatment inhibited proliferation of acute myeloid leukemia cells harboring FLT3 exon 14 insertion (FLT3-ITD) in culture (PMID: 31992353). | 31992353 |
| FLT3 exon 14 ins | acute myeloid leukemia | 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 |
| 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 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT02343939 | Phase Ib/II | Decitabine Cytarabine + Daunorubicin Entospletinib | Entospletinib Monotherapy and in Combination With Chemotherapy in Adults With Acute Myeloid Leukemia (AML) | Terminated | USA | CAN | 1 |
| NCT01799889 | Phase II | Entospletinib | A Phase 2 of Entospletinib in Subjects With Relapsed or Refractory Hematologic Malignancies | Terminated | USA | CAN | 0 |
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