Which medications in the drug class IDH Inhibitors are used in the treatment of Acute Myeloid Leukemia (AML)?

Updated: May 26, 2020
  • Author: Karen Seiter, MD; Chief Editor: Emmanuel C Besa, MD  more...
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Answer

IDH Inhibitors

Clinical trials of inhibitors of isocitrate dehydrogenase (IDH) demonstrated decreased 2-hydroxyglutarate (2-HG) levels and induced myeloid differentiation in vitro and in vivo in mouse xenograft models of IDH mutated AML.

Enasidenib (Idhifa)

Enasidenib is a small molecule inhibitor of IDH-2 enzyme. Enasidenib targets mutant IDH2 variants (ie, R140Q, R172S, and R172K) at ~40-fold lower concentrations than the wild-type enzyme in vitro. It is indicated for adults with relapsed or refractory IDH2-mutated AML.

Ivosidenib (Tibsovo)

IDH1 inhibitor; inhibits selected IDH1 R132 mutants at much lower concentrations than wild-type IDH1 in vitro. In blood samples from patients with AML with mutated IDH1, ivosidenib decreased 2-HG levels ex vivo, reduced blast counts, and increased percentages of mature myeloid cells. It is indicated for patients with susceptible IDH1 mutations who have relapsed or refractory AML. It is also indicated for newly-diagnosed IDH1-mutated AML in patients aged 75 y or older, or patients who have comorbidities that preclude use of intensive induction chemotherapy.


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