Enzomenib enantiomer

Enzomenib enantiomer (DSP-5336 enantiomer) is an enantiomer of Enzomenib. Enzomenib (DSP-5336) is an orally active Menin inhibitor ( IC₅₀ =1.4 nM, K d =6.0 nM). Enzomenib disrupts the interaction between Menin and KMT2A/MLL fusion proteins, specifically inhibits the expression of leukemia driver genes such as HOX/MEIS1, and upregulates ITGAM. Enzomenib effectively induces cell differentiation, inhibits tumor cell proliferation, and suppresses primitive cell colony formation. Enzomenib reduces disease burden and prolongs survival, but causes adverse reactions including differentiation syndrome and QTc interval prolongation. Enzomenib is used for research on relapsed/refractory acute myeloid leukemia, acute lymphoblastic leukemia, and other hematologic malignancies with mixed lineage leukemia ( MLL ) rearrangements or NPM1 mutations ^{[1] [2] [3]}.

References:
[1]. Chen T, et al. Clinical Integration of Menin Inhibitors in AML: Evolving Data and Therapeutic Perspectives. Oncol Res. 2026;34(3):4. Published 2026 Feb 24.
[2]. Daver N, et al. Phase 1/2, Open-Label, Dose Escalation, Dose Expansion Study of Menin Inhibitor DSP-5336 in Adult Patients (pts) with Acute Leukemia with and without Mixed-Lineage Leukemia (MLL)-Rearrangement or Nucleophosmin 1 (NPM1) Mutation[J]. Blood, 2021, 138: 4431.
[3]. Eguchi K, et al. Preclinical evaluation of a novel orally bioavailable menin-MLL interaction inhibitor, DSP-5336, for the treatment of acute leukemia patients with MLL-rearrangement or NPM1 mutation[J]. Blood, 2021, 138: 3339.