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Association details:
| Biomarker: | NPM1 mutation |
|---|---|
| Cancer: | Acute Myelogenous Leukemia |
| Drug: | ziftomenib (KO-539) (Menin-MLL inhibitor) + birabresib (OTX015) (BRD4 inhibitor, BRD2 inhibitor, BRD3 inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
Clinical-Stage Menin Inhibitor KO-539 Is Synergistically Active with Multiple Classes of Targeted Agents in KMT2A-r and NPM1-Mutant AML Models
Published date:
11/04/2021
Excerpt:
Notably, co-treatment (in vitro) with KO-539 in combination with venetoclax, OTX015 (pan-BET inhibitor) or abemaciclib (CDK6 inhibitor) for 72 to 96 hours induced synergistic loss of viability in cultured cell lines and PD AML cells from both MLL-r and NPM1c AML...These preclinical findings highlight the molecular correlates of anti-AML efficacy of KO-539 and demonstrate potentially synergistic KO-539-based combinations with inhibitors of BCL2, BET proteins and CDK6 against MLL-r or NPM1 mutant AML.
DOI:
10.1182/blood-2021-149831
