FIRST‐IN‐HUMAN STUDY OF THE EZH1 AND EZH2 DUAL INHIBITOR VALEMETOSTAT TOSYLATE (DS‐3201B) IN PATIENTS WITH RELAPSED OR REFRACTORY NON‐HODGKIN LYMPHOMAS

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.