Enasidenib · Idhifa, AG-221

What is Enasidenib?

Enasidenib is a small molecule inhibitor of mutant isocitrate dehydrogenase 2 (IDH2), targeting variants R140Q, R172S, and R172K. It decreases 2-hydroxyglutarate levels and induces myeloid differentiation in acute myeloid leukemia cells.

Summary written with AI from the sources listed at the end of this page.

At a glance

Also known as

Idhifa, AG-221, IDHIFA

Drug type

Small molecule

Targets

isocitrate dehydrogenase 2 (IDH2)

Mechanism

Inhibitor of isocitrate dehydrogenase 2 (IDH2)

Pathways

2-hydroxyglutarate production, myeloid differentiation, cellular proliferation

Therapy area

Oncology

Developer

Bristol Myers Squibb

In trials of

AGIO, SNDX

FDA status

Approved as Idhifa (August 1, 2017), NDA209606 · FDA label

UNII

3T1SS4E7AG

✅ FDA-approved uses

• Relapsed or refractory acute myeloid leukemia with IDH2 mutation

From the indications section of the FDA label (version of Jan 16, 2025). Read the full label for the exact wording, limitations and safety information.

🧪 Clinical trials

Trials of the companies BioRadar tracks, from ClinicalTrials.gov, most advanced phase first.

Conditions studied

Hematologic Neoplasms

Other drugs acting on IDH2

Sources

• FDA label (DailyMed)
• FDA label Idhifa (2025-01-16), indications
• NCI Thesaurus
• ClinicalTrials.gov NCT01915498
• ClinicalTrials.gov NCT03013998

Updated Oct 3, 2026.