IDH1/2 inhibitor
Mutant IDH1/IDH2 inhibitor
- ↓ 2-hydroxyglutarate (2-HG), the product of the mutant enzyme's neomorphic activity
- Falling 2-HG restores normal DNA/histone demethylation → the tumor differentiates
- Only useful where an IDH mutation is demonstrated
- Blocks the MUTANT IDH1/IDH2 enzyme, whose neomorphic activity makes 2-hydroxyglutarate
- Falling 2-HG restores normal DNA and histone demethylation, so the tumor differentiates
- Only useful where an IDH mutation has been demonstrated
Drugs with this mechanism (1)
- Vorasidenib — Brain-penetrant dual mutant-IDH inhibitor for low-grade diffuse glioma after surgery.
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