Tazemetostat, also known as EPZ-6438 and E7438, is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. EPZ-6438 induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells. Treatment of xenograft-bearing mice with EPZ-6438 leads to dose-dependent regression of MRTs with correlative diminution of intratumoral trimethylation levels of lysine 27 on histone H3, and prevention of tumor regrowth after dosing cessation.
1467052-84-1 (HCl) 1467052-75-0 (HBr) 1403254-99-8 (free base) Tazemetostat mesylate