Valemetostat Tosilate: First Approval

Abstract

Valemetostat tosilate (valemetostat; EZHARMIA®), a selective dual inhibitor of histone-lysine N-methyltransferases enhancer of zeste homolog 1 and 2 (EZH1/2), is being developed by Daiichi Sankyo Company, Ltd for the treatment of various haematological malignancies and solid tumours, including types of non-Hodgkin lymphomas (NHL). Valemetostat was approved in Japan in September 2022 for the treatment of patients with relapsed or refractory adult T-cell leukaemia/lymphoma (R/R ATL), a subtype of NHL. This article summarizes the milestones in the development of valemetostat leading to this first approval for R/R ATL.