Optimizing next-generation AML therapy: activity of mutant IDH2 inhibitor AG-221 in preclinical models
D Thomas, R Majeti - Cancer discovery, 2017 - AACR
D Thomas, R Majeti
Cancer discovery, 2017•AACRAG-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 …
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 …
Abstract
Summary: 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. Cancer Discov; 7(5); 459–61. ©2017 AACR.
See related article by Yen et al., p. 478.
See related article by Shih et al., p. 494.
AACR
