# Menin inhibitors

Source: https://onco.cc/technologies/menin-inhibitors/  
OnCo record `menin-inhibitors` (Technology). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

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.

## Fields

- Kind: Technology
- Status: approved
- Last checked: 2026-09-04
- Principle: Small molecules occupy the KMT2A-binding pocket of menin, displacing the complex from chromatin and forcing leukaemic blasts to differentiate.
- Since: 2024
- 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

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/Menin
- Wikipedia: https://en.wikipedia.org/wiki/Menin

## Connected records

- cancers: [Acute lymphoblastic leukaemia](https://onco.cc/cancers/all-leukemia/), [Acute myeloid leukaemia](https://onco.cc/cancers/aml/)
- fronts: [Targeted Therapy](https://onco.cc/fronts/targeted-therapy/)
- targets: [Menin](https://onco.cc/targets/menin/)
- drugs: [Revumenib](https://onco.cc/drugs/revumenib/), [Ziftomenib](https://onco.cc/drugs/ziftomenib/)

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