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Ref Type
Authors Alan H. Shih, Kaitlyn R Shank, Cem Meydan, Andrew M. Intlekofer, Patrick Ward, Craig B. Thompson, Ari M Melnick, Jeremy Travins, Kim Straley, Camelia Gliser, Katherine Yen, and Ross L Levine
Title AG-221, a Small Molecule Mutant IDH2 Inhibitor, Remodels the Epigenetic State of IDH2-Mutant Cells and Induces Alterations in Self-Renewal/Differentiation in IDH2-Mutant AML Model in Vivo
Journal Blood
Abstract Text Blood Dec 2014, 124 (21) 437


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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FLT3 Y599_D600insSTDNEYFYVDFREYEY IDH2 R140W acute myeloid leukemia predicted - sensitive Enasidenib + Quizartinib Preclinical Actionable In a preclinical study, the combination of Enasidenib (AG-221) and Quizartinib (AC220) stimulated leukemic cell differentiation and reduced leukemic cell self-renewal in an acute myeloid leukemia mouse model simultaneously expressing IDH2 R140Q and a FLT3-ITD mutation (Blood Dec 2014, 124 (21) 437). detail...