ivosidenib + enasidenib

Ivosidenib + enasidenib is a combination of two orally administered, small molecule inhibitors targeting distinct mutant isocitrate dehydrogenase enzymes. Ivosidenib selectively inhibits mutant isocitrate dehydrogenase 1 (mIDH1), while enasidenib targets mutant isocitrate dehydrogenase 2 (mIDH2). Both drugs lower levels of the oncometabolite 2-hydroxyglutarate, which accumulates due to IDH mutations in acute myeloid leukemia (AML), disrupting cellular differentiation. By inhibiting their respective mutant enzymes, these agents restore differentiation of myeloid blasts and reduce leukemic cell burden. As individual agents, both are approved for relapsed/refractory AML with specific IDH mutations; combinations (not co-formulated) are investigated mainly in clinical trials, particularly as adjuncts to intensive chemotherapy in newly diagnosed mIDH1/2 AML patients[1][4][8][2].

Brand names

Tibsovo + Idhifa

Other names

ivosidenib + enasidenibIDH1 inhibitor + IDH2 inhibitor