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Drug intelligence / Profile preview
balomenib + itraconazole
- Development stage
- Unknown
- Lead developer
- Eilean Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
**balomenib + itraconazole** is a combination of balomenib (ZE63-0302), a novel oral small molecule inhibitor of the menin-KMT2A interaction, and itraconazole, a triazole antifungal agent. Balomenib is designed to target leukemias characterized by KMT2A rearrangement (KMT2Ar) and NPM1-mutated acute myeloid leukemia (AML), disrupting the oncogenic menin-KMT2A protein-protein interaction central to leukemogenesis. It possesses a favorable safety profile compared to earlier menin inhibitors, displays reduced susceptibility to resistance mutations (notably "hot spot" menin mutations), and lacks significant cardiac toxicity and cytochrome P450 3A4 metabolism involvement. Itraconazole is an established inhibitor of fungal ergosterol synthesis and is sometimes used in oncology for its effect on the hedgehog signaling pathway and as a pharmacokinetic booster for drugs metabolized by CYP3A4[1][2][4][5][7]. The combination is experimental and may be used in research settings to assess pharmacokinetic interactions or to enhance balomenib exposure.
- Other names
- balomenib + itraconazole
02
Targets
CYP3A4 (Cytochrome P450 3A4)MEN1 (Menin)CYP51A1 (Sterol 14α-demethylase)
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