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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.
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.
Small molecules occupy the KMT2A-binding pocket of menin, displacing the complex from chromatin and forcing leukaemic blasts to differentiate.
Query for this technology: (TITLE:"Menin inhibitors" OR ABSTRACT:"Menin inhibitors") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Menin inhibitors, not a curated reading list.
Shares MEIS1, HOXA9, Ziftomenib, Revumenib.
Shares MEIS1, HOXA9, Ziftomenib, Revumenib.
Shares MEIS1, HOXA9, Ziftomenib, Revumenib.
Shares Ziftomenib, Revumenib, NPM1-mutated and KMT2A-rearranged acute myeloid leukaemia, Menin.
Shares Revumenib, NPM1-mutated and KMT2A-rearranged acute myeloid leukaemia, Menin, Infant acute lymphoblastic leukaemia (KMT2A-rearranged, under one year).
Shares Ziftomenib, Revumenib, NPM1-mutated and KMT2A-rearranged acute myeloid leukaemia, Menin.
Shares Revumenib, Menin, Acute lymphoblastic leukaemia, Acute myeloid leukaemia.
Shares Ziftomenib, NPM1-mutated and KMT2A-rearranged acute myeloid leukaemia, Menin, Acute myeloid leukaemia.