Drug intelligence / Profile preview

LH-1802

Development stage
Phase 1
Lead developer
Jiangsu Lianhuan Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

LH-1802 is an orally bioavailable small molecule inhibitor of the Menin-KMT2A (formerly MLL1) protein-protein interaction. Developed by Jiangsu Lianhuan Pharmaceutical, it is currently in Phase 1 clinical development for the treatment of relapsed or refractory acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS). The therapeutic rationale focuses on patients with KMT2A rearrangements (KMT2Ar) or NPM1 mutations, where the Menin-KMT2A complex drives the expression of HOXA and MEIS1 genes, maintaining a leukemic state. By competitively binding to Menin, LH-1802 disrupts this complex, leading to the downregulation of leukemogenic genes and inducing the differentiation of myeloid blasts.

02

Targets

MEN1 (Menin)KMT2A

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