• Alias: AG-221 mesylate; AG-221
    • An orally available inhibitor of specific mutant forms of the mitochondrial enzyme IDH2 that specifically inhibits various mutant forms of IDH2, including the IDH2 variants R140Q, R172S, and R172K, which inhibits the formation of 2HG. This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH2-expressing tumor cells.
    • FDA approved for relapsed, refractor acute myeloid leukemia with IDH2 mutation
    • Recommended dose: 100 mg PO daily until disease progression
    • Half-life: 137 hours (â™6 days)
    • Common side effects: Hypocalcemia, hypokalemia, nausea, diarrhea, d appetite, dysgeusia, hyperbilirubinemia, cytokine release syndrome, tumor lysis
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