Skip to search formSkip to main contentSkip to account menu

AG-221

Known as: IDH2 Inhibitor AG-221 
An orally available inhibitor of isocitrate dehydrogenase type 2 (IDH2), with potential antineoplastic activity. Upon administration, AG-221… 
National Institutes of Health

Related topics

Related topics

3 relations

Broader (2)

AminopyridinesTriazines
NCIt Antineoplastic Agent Terminology

Papers overview

Semantic Scholar uses AI to extract papers important to this topic.
2020
2020
Molecular modeling studies to discover novel mIDH2 inhibitors with high selectivity for the primary and secondary mutants
2019
2019
Treating leukemia: differentiation therapy for mIDH2 AML
2018
2018
Mutant IDH (mIDH) inhibitors, ivosidenib or enasidenib, with azacitidine (AZA) in patients with acute myeloid leukemia (AML).
7042Background: Ivosidenib (IVO; AG-120) and enasidenib (ENA; AG-221) are oral inhibitors of mIDH1 and mIDH2 proteins. In vitro… 
2017
2017
Enasidenib Monotherapy Is Effective and Well-Tolerated in Patients with Previously Untreated Mutant- IDH2 (m IDH2) Acute Myeloid Leukemia (AML)
Background: Enasidenib (AG-221) is an oral, selective inhibitor of mIDH2 proteins. Results from the AG221-C-001 phase 1/2 dose… 
2016
2016
Enasidenib (AG-221), a Potent Oral Inhibitor of Mutant Isocitrate Dehydrogenase 2 (IDH2) Enzyme, Induces Hematologic Responses in Patients with Myelodysplastic Syndromes (MDS)
Introduction : IDH2 mutations (m IDH2 ) are recurrent in ~5% of patients (pts) with MDS and ~15% of pts with acute myeloid… 
Review
2016
Review
2016
The Evolving Landscape in the Development of Isocitrate Dehydrogenase Mutant Inhibitors.
Isocitrate dehydrogenase (IDH) is a metabolic enzyme that converts isocitrate to α-ketoglutarate (α-KG). Genetic gain-of-function… 
Review
2015
Review
2015
IDH2 inhibition in AML: Finally progress?
2014
2014
AG-221, an Oral, Selective, First-in-Class, Potent IDH2-R140Q Mutant Inhibitor, Induces Differentiation in a Xenotransplant Model
Somatic point mutations in the active site of IDH (isocitrate dehydrogenase) 1 and IDH2 genes are observed in acute myeloid… 
2014
2014
Evaluation of Pharmacokinetic-Pharmacodynamic (PKPD) Relationship of an Oral, Selective, First-in-Class, Potent IDH2 Inhibitor, AG-221, from a Phase 1 Trial in Patients with Advanced IDH2 Mutant…
Introduction : Isocitrate dehydrogenase (IDH) is a critical enzyme in the citric acid cycle, catalyzing the oxidative… 
2014
2014
Abstract 3116: AG-221 offers a survival advantage in a primary human IDH2 mutant AML xenograft model
Somatic point mutations in isocitrate dehydrogenase 1/2 (IDH1/2) confer a gain-of-function in cancer cells resulting in the… 
By clicking accept or continuing to use the site, you agree to the terms outlined in our Privacy Policy (opens in a new tab), Terms of Service (opens in a new tab), and Dataset License (opens in a new tab)