EZM8266

**EZM8266** is a first-in-class, potent, selective, and orally bioavailable small-molecule inhibitor of EHMT2 (also known as G9a or GLP), a histone methyltransferase that catalyzes H3K9 methylation and plays a role in epigenetic regulation. Developed by Epizyme (now a subsidiary of Ipsen), it was investigated primarily as a novel therapy for **sickle cell disease** (SCD) by inducing fetal hemoglobin production through EHMT2 inhibition, with potential extension to oncology given EHMT2's role as a cancer target. Preclinical studies supported IND-enabling work, but development was halted due to toxicology findings in preclinical studies.[1][3][5][7][9]