Article
Enasidenib in mutant IDH2 relapsed or refractory acute myeloid leukemia.
Blood - 10 Aug 2017
Stein Eytan M, DiNardo Courtney D, Pollyea Daniel A, Fathi Amir T, Roboz Gail J, Altman Jessica K, Stone Richard M, DeAngelo Daniel J, Levine Ross L, Flinn Ian W, Kantarjian Hagop M, Collins Robert, Patel Manish R, Frankel Arthur E, Stein Anthony, Sekeres Mikkael A, Swords Ronan T, Medeiros Bruno C, Willekens Christophe, Vyas Paresh, Tosolini Alessandra, Xu Qiang, Knight Robert D, Yen Katharine E, Agresta Sam, de Botton Stephane, Tallman Martin S
Abstract excerpt
Recurrent mutations in isocitrate dehydrogenase 2 (IDH2) occur in ∼12% of patients with acute myeloid leukemia (AML). Mutated IDH2 proteins neomorphically synthesize 2-hydroxyglutarate resulting in DNA and histone hypermethylation, which leads to blocked cellular differentiation. Enasidenib (AG-221/CC-90007) is a first-in-class, oral, selective inhibitor of mutant-IDH2 enzymes. This first-in-human phase 1/2 study...
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