Revumenib sesquifumarateProduct ingredient for Revumenib

Abnormal gene rearrangements at chromosome locus 11q23, called KMT2A rearrangements or translocations, are present in 5%-10% of patients with acute leukemias and are the sole genetic aberration found in the majority of infant acute lymphoblastic leukemia cases.¹ Aberrant KMT2A is associated with the upregulation of leukemogenic transcription pathways, notably those involving HOXA genes and their co-factor MEIS1. Menin is a scaffold protein that interacts with both the wild-type and rearranged KMT2A, which is crucial for KMT2A activity and the maintenance of HOXA expression and leukemogenesis.¹

Revumenib is an oral small molecule menin inhibitor that prevents the interaction between menin and aberrant KMT2A. It was approved by the FDA in November 2024 for the treatment of leukemia with KMT2A aberrations,^3,2 becoming the first menin inhibitor to receive FDA approval.⁵ In October of 20225, it was approved for myeloid leukemia patients with nucleophosmin 1 (NPM1) mutations. ⁷