Revumenib CAS# 2169919-21-3 N-乙基-2-[[4-[7-[[[反式-4-[(乙磺酰基)氨基]环己基]甲基]-2,7-二氮杂螺[3.5]非-2-基]-5-嘧啶基]氧基]-5-氟-N-(1-甲基乙基)苯甲酰胺

Revumenib (SNDX-5613) is a potent, orally bioavailable small-molecule inhibitor of the menin–KMT2A (MLL) protein-protein interaction critical in certain acute leukemias. In preclinical binding studies, it disrupted the menin–KMT2A interaction with low-nanomolar potency (IC₅₀ ≈ 2–20 nM), downregulating oncogenic HOXA/MEIS1 transcription. In human AML cell lines with KMT2A rearrangements or NPM1 mutations, revumenib inhibited proliferation (IC₅₀ ~12–24 nM) and reversed leukemogenic gene expression. In xenograft models, oral dosing produced dose-dependent suppression of leukemic burden and significant survival benefits, with minimal off-target activity, supporting its development for aggressive leukemia subtypes.