2019 Medicinal Chemistry Reviews

Volume 54, Chapter 7
IDH Inhibitors for the Treatment of IDH-Mutated Cancer
Lenny Dang, Brandon Nicolay, Zenon Konteatis

1. Introduction
2. Biochemistry of IDH Enzymes
3. Discovery of Gain-of-Function IDH Mutations
4. Cancer Biology of Oncometabolite 2-HG
5. Mutant IDH2 Inhibitors: AGI-6780, AG-221 (Enasidenib)
6. Mutant IDH1 Inhibitors: AG-881 (Vorasidenib), AGI-5198, ML309, AG-120 (Ivosidenib), IDH889, IDH305, LY 3410738, FT-2102 (Olutasidenib), BAY 1436032, MRK-A
7. Acquired Drug Resistance and Future Directions

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