First-in-Human Study of the EZH1/2 Dual Inhibitor Valemetostat in Relapsed or Refractory Non-Hodgkin Lymphoma (NHL) - Updated Results Focusing on Adult T-Cell Leukemia-Lymphoma (ATL)

Introduction: Enhancer of zeste homolog 2 (EZH2) and EZH1 are alternative subunits of polycomb repressive complex 2 that catalyze the tri-methylation of lysine 27 residue of histone H3. This histone modification epigenetically regulates gene expression and may play an important role in tumor progression. Valemetostat (DS-3201) is a potent and highly specific orally bioavailable dual inhibitor of EZH2 and EZH1 demonstrating anti-tumor activity...