molecules of the month


oral menin-MLL1/KMT2A inhibitor

Ph. I/II for R/R leukemia, CRC & solid tumors

SBDD and opt. of known Menin inhibitor fragment

Nature, March 15, 2023

Vitae, Madison, NJ / Syndax, Waltham, MA

revumenib, oral menin-KMT2A inhibitor, Ph. I/II for r/r leukemia, CRC & solid tumors, discovery not disclosed, Nature, March 15, 2023, VITAE, MADISON, NJ / SYNDAX, WALTHAM, MA
7 mins read

Revumenib: a novel Menin-MLL1 inhibitor in Ph. II for AML. Acute myeloid leukemia (AML) remains difficult to treat, with few novel therapies approved in the last three decades. A subset of these aggressive leukemias, mixed lineage leukemias, are driven by fusions between the MLL1 gene (“Mixed Lineage Leukemia”, or KMT2A) and more than 80 different fusion partners. MLL fusion proteins form part of a protein complex that upregulates the transcription of the leukemogenic HOXA and MEIS1 genes, which drive proliferation and block differentiation of hematopoietic cells, ultimately leading to the acute lymphocytic leukemia (ALL) or acute myelogenous leukemia (AML). The histone lysine methyltransferase Menin is a key member of the complex, connecting transcription factors to chromatin. Hence, targeting the protein-protein interaction between Menin and MLL could…

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