By restoring the expression of tumor suppressor genes silenced by abnormal epigenetic alterations, many epigenetic inhibitors—including EPZ-6438 (tazemetostat), a selective inhibitor of the histone methyltransferase EZH2—and RG108, a non-nucleoside inhibitor of DNA methyltransferases (DNMTs)—have shown promising efficacy in preclinical cancer models. The gene discussed is EZH2; the disease is cancer.