RCZY-843 / Rongchang Pharma - LARVOL DELTA

RCZY-843: A potential best-in-class, second-generation menin-MLL inhibitor engineered to overcome clinically observed menin-mutation-mediated resistance, with superior preclinical efficacy and safety in acute leukemia models (AACR 2026) - "Fluorescence polarization assays further confirm its potent disruption of the menin-MLL interaction in the presence of clinically observed resistance mutations (M327I/V, G331R, T349M) with substantially lower IC₅₀ values than approved or clinical-stage menin inhibitors (SNDX-5613, KO-539, JNJ-75276617). Compared to SNDX-5613, RCZY-843 further demonstrates favorable PK/PD characteristics—including stronger and more durable MEIS1 mRNA suppression—along with good in vivo tolerability, and a wide therapeutic window, as supported by a 14-day rat DRF toxicity study. In conclusion, RCZY-843 is a potential best-in-class, second-generation menin-MLL inhibitor capable of overcoming MEN1 mutation-mediated acquired resistance, with robust preclinical efficacy and a favorable safety profile for the treatment of KMT2A-rearranged/NPM1-mutant acute leukemias."

Preclinical • Hematological Malignancies • Leukemia • Oncology • KMT2A • MEIS1 • MEN1 • NPM1