Valemetostat — Investigational Agent

Other · Phase 2 · Daiichi Sankyo

Mechanism of Action

An oral, dual inhibitor of EZH1 and EZH2, the catalytic subunits of the PRC2 complex that trimethylate histone H3K27. Simultaneous EZH1/EZH2 blockade more completely relieves PRC2-mediated silencing of tumor-suppressor genes than EZH2-selective inhibition, driving apoptosis in T-cell lymphomas and adult T-cell leukemia/lymphoma.

Investigational Indications

Key Trials