Balomenib (ZE63-0302) is an orally bioavailable menin-KMT2A interaction inhibitor. Balomenib disrupts menin-KMT2A binding, reverses aberrant HOX gene expression. Balomenib inhibits Meis1 mRNA expression in KMT2A-rearranged acute myeloid leukemia cells. Balomenib can be used for the research of leukemia [1].
In Vitro, Balomenib inhibits Meis1 mRNA expression in MOLM‑13 cells (KMT2Ar/MLLr AML cell line) in an exposure‑dependent manner, with peak inhibition at Cmax in an ex vivo plasma inhibitory assay (PIA)[1]. Balomenib disrupts the binding of menin to KMT2A to reverse aberrant HOX gene overexpression driven by menin‑KMT2A interaction in KMT2Ar and NPM1c mutant AML cells[1].
References:
[1]. Burd A, et al. A randomized placebo-controlled Phase 1 trial in healthy volunteers investigating safety, pharmacokinetics and pharmacodynamics of a novel menin inhibitor, balomenib (ZE63-0302): Interim analysis. Blood. 2025;146 Suppl 1:5067.
In Vitro, Balomenib inhibits Meis1 mRNA expression in MOLM‑13 cells (KMT2Ar/MLLr AML cell line) in an exposure‑dependent manner, with peak inhibition at Cmax in an ex vivo plasma inhibitory assay (PIA)[1]. Balomenib disrupts the binding of menin to KMT2A to reverse aberrant HOX gene overexpression driven by menin‑KMT2A interaction in KMT2Ar and NPM1c mutant AML cells[1].
References:
[1]. Burd A, et al. A randomized placebo-controlled Phase 1 trial in healthy volunteers investigating safety, pharmacokinetics and pharmacodynamics of a novel menin inhibitor, balomenib (ZE63-0302): Interim analysis. Blood. 2025;146 Suppl 1:5067.