enasidenib (idhifa) Report issue

Small molecule Orphan Drug FDA Approved FDA First in Class Fast Track FDA Priority Review FDA
AACT DrugBank Drugs@FDA PubChem

Active Ingredient History

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  • Now
Enasidenib, aslo known as AG-221 and CC-90007, is a potent and selective IDH2 inhibitor with potential anticancer activity (IDH2 = Isocitrate dehydrogenase 2). The mutations of IDH2 present in certain cancer cells result in a new ability of the enzyme to catalyze the NAPH-dependent reduction of α-ketoglutarate to R(-)-2-hydroxyglutarate (2HG). The production of 2HG is believed to contribute to the formation and progression of cancer. The inhibition of mutant IDH2 and its neoactivity is therefore a potential therapeutic treatment for cancer. Enasidenib is an orally available, selective, potent inhibitor of the mutated IDH2 protein, making it a highly targeted investigational medicine for the potential treatment of patients with cancers that harbor an IDH2 mutation. Enasidenib has received orphan drug and fast track designations from the U.S. FDA. Enasidenib mesylate is in phase II clinical trials for Solid tumours and phase III clinical trials for the treatment of acute myeloid leukaemia.   NCATS

Chemistry

  • SMILES: CC(C)(O)CNc1nc(Nc2ccnc(c2)C(F)(F)F)nc(n1)c3cccc(n3)C(F)(F)F
  • InChIKey: DYLUUSLLRIQKOE-UHFFFAOYSA-N
  • Mol. Mass: 473.38
  • ALogP: 4.29
  • ChEMBL Molecules:
    enasidenib  
    enasidenib mesylate  
More Chemistry

Pharmacology

Drug Pricing (per unit)

United States

$628.6120 - $827.7550
More Pricing Detail

Note: This drug pricing data is preliminary, incomplete, and may contain errors.

Alternative names

2-methyl-1-(4-(6-(trifluoromethyl)pyridin-2-yl)-6-(2-(trifluoromethyl)pyridin-4-ylamino)-1,3,5-triazin-2-ylamino)propan-2-ol | 2-propanol, 2-methyl-1-((4-(6-(trifluoromethyl)-2-pyridinyl)-6-((2-(trifluoromethyl)-4-pyridinyl)amino)-1,3,5-triazin-2-yl)amino)- | ag221 | ag-221 | enasidenib | enasidenib mesylate | idhifa

Organizations (34)

Research & Development (33)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Marketing (2)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Indications (23)

Approved Indications (1)


 

Leukemia, Myeloid, Acute

Experimental Indications - Clinical Trial Phases 1-4 (23)


 

Bone Marrow Cells (Phase 2)

Cholangiocarcinoma (Phase 1/Phase 2)

Chondrosarcoma (Phase 2)

Clonal Hematopoiesis (Phase 1)

Drugs, Investigational (Phase 2)

Glioma (Phase 1/Phase 2)

Healthy Volunteers (Phase 1)

Hematologic Neoplasms (Phase 1/Phase 2)

Isocitrate Dehydrogenase (Phase 3)

Leukemia (Phase 2)

Leukemia, Biphenotypic, Acute (Phase 2)

Leukemia, Monocytic, Acute (Phase 1/Phase 2)

Leukemia, Myeloid (Phase 3)

Leukemia, Myeloid, Acute (Phase 3)

Leukemia, Myelomonocytic, Chronic (Phase 2)

Liver Diseases (Phase 1)

Lymphoma, T-Cell (Phase 1/Phase 2)

Multiple Myeloma (Phase 1/Phase 2)

Mutation (Phase 2)

Myelodysplastic Syndromes (Phase 3)

Myeloproliferative Disorders (Phase 2)

Neoplasms (Phase 1/Phase 2)

Primary Myelofibrosis (Phase 2)

Overview

  • Highest Phase: Phase 3
  • # of Trials: 38
  • # of Trial Organizations: 33

Trials by Phase

Trial Phase Start Date Organizations Indications

Feedback

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