. Author manuscript; available in PMC: 2019 Jul 26.

Published in final edited form as: Leuk Lymphoma. 2018 Feb 23;59(7):1574–1585. doi: 10.1080/10428194.2018.1430795

Table 3:

Tazemetostat Quick Profile

Drug Name	Tazemetostat
Company	Epizyme, Inc.
Other Names	E7438/ EPZ-6438
MOA (Mechanism of action)	EZH2 inhibitor, Competitive inhibition with the cofactor S-adenosyl-L-methionine (SAM)
MOR (Mechanism of resistance)	Not well characterized. In-vitro data suggests that secondary mutations in the EZH2 D1 domain (Y111 and I109) and SET domain (Y661) may confer resistance
MTD	1600mg PO BID
Schedule	800 mg PO BID
Plasma half-life	T max = 1–2 hrs., mean terminal t_1/2 = 3–5hrs
Other unique features	- Fast Track designation for EZH2 mutant DLBCL and for FL regardless of EZH2 mutation status - Orphan Drug designation for malignant rhabdoid tumors