Drug intelligence / Profile preview

EP-0108

Development stage: Unknown
Lead developer: Chengdu Easton Biopharmaceuticals
Modality: Small Molecules
Administration: Oral

Overview

EP-0108 is an orally bioavailable, highly selective small molecule inhibitor of the Menin-KMT2A (formerly MLL1) protein-protein interaction. Developed by Chengdu Easton Biopharmaceuticals, it is primarily indicated for the treatment of relapsed or refractory acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) harboring KMT2A rearrangements or NPM1 mutations. These genetic alterations lead to the recruitment of Menin to specific gene loci, driving the expression of leukemogenic genes like HOXA9 and MEIS1. By blocking this interaction, EP-0108 promotes myeloid differentiation and inhibits the proliferation of leukemia cells. It is currently in Phase 1 clinical development in China.

Targets

KMT2A

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