Valemetostat (DS-3201) is an EZH1/2 inhibitor that can be used to study relapsed/refractory peripheral T-cell lymphoma.

METHODS: Valemetostat (DS-3201) was used to treat a group of malignant lymphoma cell lines derived from EZH1+ differentiated lymphocytes at low doses (0.1-100 nM), and the expression of H3K27me3 in sensitive lymphoma cells was observed.
RESULTS valemetostat effectively inhibited H3K27me3 in sensitive lymphoma types, showing a targeted effect. [1]
METHODS: The EZH inhibitor valemetostat (0.1-1000nM) was chemically screened and derivatized using half the maximal inhibitory concentration (IC50) of EZH1/2 and cellular H3K27me3.
RESULTS valemetostat strongly and specifically inhibits EZH1 and EZH2 (IC50 < 10 nM). [2]
METHODS: Human MCL cell lines Mino, JeKo-1, and REC-1 were treated with varying concentrations of valemetostat ranging from 3000 to 0.3 nmol/L or 3000 to 100 nmol/L, respectively.
RESULTS Valemetostat at a concentration lower than 100 nmol/L significantly inhibited the growth of Mino and JeKo-1, while valemetostat at a concentration higher than 100 nmol/L inhibited the growth of REC-1. [3]

METHODS: In diffuse large B-cell lymphoma (DLBCL) cell xenograft model mice, Valemetostat (DS-3201) (25 mg/kg/50 mg/kg/100 mg/kg) was orally administered once a day to observe the tumor growth in the mice.
RESULTS Valemetostat 100 mg/kg orally once daily was associated with nearly complete tumor regression without weight loss; lower doses (25 mg/kg) slowed tumor growth. [1]
METHODS: Primary MCL cells were transplanted into 6-week-old SCID-Beige (SCIDbg) mice (CB17.Cg-Prkdc) by subcutaneous injection, and the mice were treated with valemetostat 200 mg/kg twice daily for three days. week.
RESULTS valemetostat treatment significantly inhibited tumor growth, and all valemetostat-treated mice survived to the end of the study period. [3]