4.7 Editorial Material

Optimizing Next-Generation AML Therapy: Activity of Mutant IDH2 Inhibitor AG-221 in Preclinical Models

Journal

CANCER DISCOVERY
Volume 7, Issue 5, Pages 459-461

Publisher

AMER ASSOC CANCER RESEARCH
DOI: 10.1158/2159-8290.CD-17-0270

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Funding

  1. NCI NIH HHS [R21 CA195127, R01 CA188055, K99 CA207731] Funding Source: Medline

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AG-221 or enasidenib is a first-in-class selective inhibitor of mutated isocitrate dehydrogenase 2 (IDH2) with early demonstrated clinical efficacy in acute myeloid leukemia as a single agent, yet with persistence of mutant IDH2 clones. Two articles in this issue of Cancer Discovery provide further insight into the biological activity of AG-221 in promoting differentiation of IDH2-mutant cells and reversing aberrant DNA methylation over time, and demonstrating preclinical activity in combination with a targeted FLT3 kinase inhibitor to eliminate IDH2-mutant clones. (C) 2017 AACR.

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