Last reviewed 2026-04-23 · How we verify

AG-881

Tet methylcytosine dioxygenase 2 (TET2) inhibitor

Tet methylcytosine dioxygenase 2 (TET2) inhibitor Used for Acute myeloid leukemia (AML).

At a glance

Mechanism of action

AG-881 is a potent and selective inhibitor of TET2, a key enzyme involved in DNA demethylation. Inhibition of TET2 has been shown to induce DNA hypermethylation and suppress cancer cell growth.

Approved indications

• Acute myeloid leukemia (AML)

Common side effects

• Fatigue
• Nausea
• Diarrhea

Key clinical trials

• Study of Vorasidenib and Pembrolizumab Combination in Recurrent or Progressive IDH-1 Mutant Glioma (PHASE1)
• Study of Orally Administered AG-881 in Patients With Advanced Solid Tumors, Including Gliomas, With an IDH1 and/or IDH2 Mutation (PHASE1)
• Study of AG-120 and AG-881 in Subjects With Low Grade Glioma (PHASE1)
• Phase 3 Study of Vorasidenib (S095032/AG-881) in Asian Participants With Residual or Recurrent Grade 2 Glioma With an IDH1 orIDH2 Mutation (PHASE3)
• Study of Oral LY3410738 in Patients With Advanced Hematologic Malignancies With IDH1 or IDH2 Mutations (PHASE1)
• Study of Vorasidenib (AG-881) in Participants With Residual or Recurrent Grade 2 Glioma With an IDH1 or IDH2 Mutation (INDIGO) (PHASE3)
• Vorasidenib Expanded Access Program
• A Study of Vorasidenib in Participants With Moderate or Mild Hepatic Impairment and Matched Participants With Normal Hepatic Function (PHASE1)

Primary sources

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Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• AG-881 CI brief — competitive landscape report
• AG-881 updates RSS · CI watch RSS
• Agios Pharmaceuticals, Inc. portfolio CI