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Therapy Name | Pinometostat |
Synonyms | |
Therapy Description |
Pinometostat (EPZ-5676) inhibits DOT1L histone methyltransferase activity, resulting in decreased growth of leukemia cells with MLL rearrangements (PMID: 23801631, PMID: 26645404, PMID: 29724899). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Pinometostat | EPZ-5676|EPZ5676 | DOT1L Inhibitor 3 | Pinometostat (EPZ-5676) inhibits DOT1L histone methyltransferase activity, resulting in decreased growth of leukemia cells with MLL rearrangements (PMID: 23801631, PMID: 26645404, PMID: 29724899). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
KMT2A rearrange | acute leukemia | predicted - sensitive | Pinometostat | Case Reports/Case Series | Actionable | In a Phase I trial, Pinometostat (EPZ-5676) treatment resulted in complete remission in 2 patients with KMT2A rearranged (both with t(11;19)) acute leukemia (PMID: 29724899; NCT01684150). | 29724899 |
DNMT3A mutant | acute myeloid leukemia | sensitive | Pinometostat | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Pinometostat (EPZ-5676) treatment of acute myeloid leukemia cell lines and xenografts resulted in apoptosis, cell-cycle arrest, and terminal differentiation (PMID: 27335278). | 27335278 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT02141828 | Phase I | Pinometostat | A Phase 1 Dose Escalation and Expanded Cohort Study of EPZ-5676 in the Treatment of Pediatric Patients With Relapsed/Refractory Leukemias Bearing a Rearrangement of the MLL Gene | Completed | USA | CAN | 0 |