The observation that EZH2 is often overexpressed in cancers led to the development of certain small molecule agents targeting this histone methyltransferase such as EPZ-6438 (tazemetostat), GSK2816126, and CPI-1205 [239,258]; these drugs are currently in early clinical studies reporting clinical responses with acceptable tolerability in many cancers [258,259]. Here, EZH2 is linked to cancer.