Article
Enasidenib induces acute myeloid leukemia cell differentiation to promote clinical response.
Blood - 10 Aug 2017
Amatangelo Michael D, Quek Lynn, Shih Alan, Stein Eytan M, Roshal Mikhail, David Muriel D, Marteyn Benoit, Farnoud Noushin Rahnamay, de Botton Stephane, Bernard Olivier A, Wu Bin, Yen Katharine E, Tallman Martin S, Papaemmanuil Elli, Penard-Lacronique Virginie, Thakurta Anjan, Vyas Paresh, Levine Ross L
Abstract excerpt
Recurrent mutations at R140 and R172 in isocitrate dehydrogenase 2 (IDH2) occur in many cancers, including ∼12% of acute myeloid leukemia (AML). In preclinical models these mutations cause accumulation of the oncogenic metabolite R-2-hydroxyglutarate (2-HG) and induce hematopoietic differentiation block. Single-agent enasidenib (AG-221/CC-90007), a selective mutant IDH2 (mIDH2) inhibitor, produced an overall...
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