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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 | ||||||||||||
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URL | http://www.bloodjournal.org/content/124/21/437?sso-checked=true | ||||||||||||
Abstract Text | Blood Dec 2014, 124 (21) 437 |
Molecular Profile | Treatment Approach |
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Therapy Name | Drugs | Efficacy Evidence | Clinical Trials |
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Gene | Variant | Impact | Protein Effect | Variant Description | Associated with drug Resistance |
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Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
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FLT3 exon 14 ins IDH2 R140Q | acute myeloid leukemia | predicted - sensitive | Enasidenib + Quizartinib | Preclinical | Actionable | In a preclinical study, the combination of Enasidenib (AG-221) and Vanflyta (quizartinib) 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... |