Most of the currently developed EZH2 inhibitors focus on targeting the enzymatic activity of EZH2 and exhibited antitumor activities, including Tazmestat (EPZ6438),27 CPI1205,28 GSK126,7 UNC1999,29 and EPZ005687.30 EPZ6438 has been granted approval from the US FDA for the treatment of patients with metastatic or locally advanced epithelioid sarcoma or relapsed/refractory FL. The gene discussed is EZH2; the disease is epithelioid sarcoma.