Mutant isocitrate dehydrogenase 1/2 (mIDH1/2) proteins catalyze production of the oncometabolite D‐2‐hydroxyglutarate (2‐HG). Ivosidenib and enasidenib are oral inhibitors of mIDH1 and mIDH2, respectively. An open‐label phase 1 study is… Click to show full abstract
Mutant isocitrate dehydrogenase 1/2 (mIDH1/2) proteins catalyze production of the oncometabolite D‐2‐hydroxyglutarate (2‐HG). Ivosidenib and enasidenib are oral inhibitors of mIDH1 and mIDH2, respectively. An open‐label phase 1 study is evaluating the safety and efficacy of ivosidenib or enasidenib combined with intensive induction and consolidation chemotherapy in adult patients with newly diagnosed mIDH1/2 acute myeloid leukemia (AML; NCT02632708). In this population, we characterized the pharmacokinetics (PK), pharmacodynamics (PD), and PK/PD relationships for ivosidenib and enasidenib.
               
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