IDH1/2 inhibitor
Mutant IDH1/IDH2 inhibitor
- ↓ 2-hydroxyglutarate (2-HG), the product of the mutant enzyme's neomorphic activity
- Blocks the MUTANT IDH1/IDH2 enzyme
- Falling 2-HG restores normal DNA/histone demethylation → the tumor differentiates
- Only useful where an IDH mutation is demonstrated
Drugs with this mechanism (1)
- Vorasidenib — Brain-penetrant dual mutant-IDH inhibitor for low-grade diffuse glioma after surgery.
Self-check
- Which metabolite falls with mutant IDH inhibition?
2-hydroxyglutarate (2-HG). - What must be demonstrated for an IDH inhibitor to be useful?
An IDH mutation.
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