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Menin Inhibitor

Menin-KMT2A Disruption

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Source: *KMT2A = KMT2A rearrangement or KMT2A wildtype; Adapted from: Uckelmann HJ, et al. Presented at ASH Annual Meeting, 2018.

Menin is a scaffold protein, and its binding to KMT2A leads to transcriptional activation of leukemogenic genes such as HOX and MEIS1. When revumenib is introduced, it fits into the binding pocket of menin and displaces KMT2A. In disrupting the binding interaction, the HOX and MEIS genes are turned off and leukemic cell growth is halted.

View the mechanism of action below:

 


References:

  1. Li X, Song Y. J Hematol Oncol. 2021;14:56.