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Enasidenib is an oral, reversible, selective inhibitor of mutated isocitrate dehydrogenase (IDH) 2.1,2 In vitro studies suggest that the oncometabolite 2-hydroxyglutarate (2-HG), which is present at high levels in patients with IDH mutations,3-5 may drive epigenetic changes that block normal cellular differentiation, leading to a cancerous state.2,4 As demonstrated in preclinical studies, enasidenib binds and inhibits the mutant IDH2 enzyme that is responsible for the accumulation of 2-HG.2
Enasidenib Hypothesized Mechanism of Action
Enasidenib is a selective inhibitor of mutant IDH2 and has been hypothesized to reduce 2-HG levels which may restore DNA demethylation in acute myeloid leukemia.
1st line with an IDH2 Mutation
Relapsed/Refractory with an IDH2 Mutation
IDH2 mutations occur in various cancers and occur in approximately 8% to 19% of patients with AML.5-7 Preclinical data suggest that enasidenib may have clinical activity in IDH2-mutant AML through the reduction of 2-HG levels and the induction of blast differentiation.2 In vitro studies have shown that enasidenib may reduce 2-HG levels by > 90%, reverse histone and DNA hypermethylation, and induce differentiation in leukemia cell models.2 In a primary human mutant IDH2 AML xenograft model, enasidenib reduced 2-HG levels and induced dose-dependent proliferation and differentiation.2