Drug intelligence / Profile preview

bleximenib + azacitidine

Development stage
Phase 1
Lead developer
Johnson & Johnson
Modality
Small Molecules
Administration
Oral, Intravenous, Subcutaneous
01

Overview

**Bleximenib + azacitidine** is an investigational combination therapy for acute myeloid leukemia (AML), specifically for patients with *KMT2A* gene rearrangements or *NPM1* gene mutations who are ineligible for intensive chemotherapy or have relapsed/refractory disease. Bleximenib is a selective oral menin inhibitor (JNJ-75276617) that targets the interaction between menin and histone-lysine N-methyltransferase 2A (KMT2A/MLL1), disrupting oncogenic epigenetic signaling critical for leukemogenesis in these AML subtypes[1][2][3][5]. Azacitidine is a hypomethylating agent that inhibits DNA methyltransferase, promoting re-expression of tumor suppressor genes and apoptosis in malignant cells. This combination, often studied with venetoclax as a triplet, has shown promising anti-leukemic activity and tolerability in early and ongoing trials.

02

Targets

DNMT (DNA methyltransferase)MEN1 (Menin)

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