FIRST‐IN‐HUMAN STUDY OF THE EZH1 AND EZH2 DUAL INHIBITOR VALEMETOSTAT TOSYLATE (DS‐3201B) IN PATIENTS WITH RELAPSED OR REFRACTORY NON‐HODGKIN LYMPHOMAS
Kenji Ishitsuka, Koji Izutsu, D Maruyama, Shinichi Makita, Eric D. Jacobsen, Steven M. Horwitz, Shigeru Kusumoto, Pamela B. Allen, Pierluigi Porcu, Yoshitaka Imaizumi, Nobuhiko Yamauchi, Satoko Morishima, Toyotaka Kawamata, Francine M. Foss, Atae Utsunomiya, Kisato Nosaka, Gul Serbest, Kazunobu Kato, Nobuaki Adachi, Kunihiro Tsukasaki, Kensei Tobinai
Abstract
Abstract Introduction: Enhancer of zeste homolog 2 (EZH2) and its close homolog, EZH1, catalyze the attachment of 3 methyl groups to histone H3 at lysine 27. Altered EZH2 expression is implicated in the etiology of non‐Hodgkin lymphomas (NHLs). Valemetostat tosylate (DS‐3201b; valemetostat) is a novel, potent, and selective dual inhibitor of EZH2 and EZH1. This article is protected by copyright. All rights reserved. This article is protected by copyright. All rights reserved.