{"entity":{"id":"menin-inhibitors","kind":"technology","name":"Menin inhibitors","aka":[],"tldr":"Pills that break the interaction between menin and the KMT2A protein that acute leukaemias with KMT2A rearrangements or NPM1 mutations depend on; revumenib was the first approved, in 2024.","summary":"About one in ten acute leukaemias carries a KMT2A (MLL) rearrangement and around a third of adult acute myeloid leukaemia has an NPM1 mutation; both rely on menin binding KMT2A to keep leukaemia genes switched on. Revumenib (Revuforj) was approved in 2024 for relapsed or refractory KMT2A-rearranged acute leukaemia, with ziftomenib following in NPM1-mutant disease; differentiation syndrome is the class toxicity and MEN1 mutations cause resistance. Combinations with venetoclax and azacitidine are in trials.","status":"approved","asOf":"2026-09-04","wikipedia":"https://en.wikipedia.org/wiki/Menin","links":[{"label":"Wikipedia","url":"https://en.wikipedia.org/wiki/Menin"}],"tags":[],"related":[],"cancers":["aml","all-leukemia"],"sections":["targeted-therapy"],"technologies":[],"targets":["menin"],"drugs":["revumenib","ziftomenib"],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"principle":"Small molecules occupy the KMT2A-binding pocket of menin, displacing the complex from chromatin and forcing leukaemic blasts to differentiate.","strengths":["First targeted drugs for KMT2A-rearranged leukaemia","Oral, with responses in heavily pretreated patients"],"limitations":["Differentiation syndrome and QT prolongation","Acquired MEN1 mutations cause resistance"],"since":2024},"route":"/technologies/menin-inhibitors/","neighbours":{"cancer":[{"id":"all-leukemia","kind":"cancer","name":"Acute lymphoblastic leukaemia","route":"/cancers/all-leukemia/"},{"id":"aml","kind":"cancer","name":"Acute myeloid leukaemia","route":"/cancers/aml/"},{"id":"aml-paediatric","kind":"cancer","name":"Acute myeloid leukaemia in children","route":"/cancers/aml-paediatric/"},{"id":"all-infant","kind":"cancer","name":"Infant acute lymphoblastic leukaemia (KMT2A-rearranged, under one year)","route":"/cancers/all-infant/"},{"id":"leukaemia","kind":"cancer","name":"Leukaemia (all types)","route":"/cancers/leukaemia/"},{"id":"aml-npm1-kmt2a","kind":"cancer","name":"NPM1-mutated and KMT2A-rearranged acute myeloid leukaemia","route":"/cancers/aml-npm1-kmt2a/"}],"section":[{"id":"targeted-therapy","kind":"section","name":"Targeted Therapy","route":"/fronts/targeted-therapy/"}],"target":[{"id":"hoxa9","kind":"target","name":"HOXA9","route":"/targets/hoxa9/"},{"id":"meis1","kind":"target","name":"MEIS1","route":"/targets/meis1/"},{"id":"menin","kind":"target","name":"Menin","route":"/targets/menin/"}],"drug":[{"id":"revumenib","kind":"drug","name":"Revumenib","route":"/drugs/revumenib/"},{"id":"ziftomenib","kind":"drug","name":"Ziftomenib","route":"/drugs/ziftomenib/"}],"trial":[{"id":"beat-aml-master-trial","kind":"trial","name":"Beat AML Master Trial","route":"/trials/beat-aml-master-trial/"}]}}