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Showing posts with the label KMT2A

Hutchmed expanded its presence in blood cancers by developing a Menin inhibitor

 HUTCHMED (formerly Hutchison MediPharma) has introduced its Menin-MLL inhibitor HMPL-506 into a phase 1 trial, aiming to broaden its footprint in hematological malignancies. The company filed the IND application for HMPL-506 in January 2024 in China.  Menin binds to KMT2A, activating leukemogenic genes like HOX and MEIS1. However, when a Menin inhibitor binds to the pocket of menin and displaces KMT2A, it deactivates HOX and MEIS genes, halting the growth of leukemic cells. Targeting Menin Currently, HUTCHMED possesses several drug candidates targeting SYK, PI3Kδ, IDH1/2, BTK, CD47, and Menin, in addition to the in-licensed EZH2 inhibitor tazemetostat, all of which are part of the pipeline for blood cancers. HUTCHMED Pipeline in 2024Q1 HMPL-506 MLL gene rearrangements (MLL-r, also known as KMT2A) are found in 5%-10% of acute leukemias and are linked to a poorer prognosis. On the other hand, nucleophosmin 1 mutations (NPM1m) are the most frequent genetic changes seen in acute myeloid l