EZH2 has been actively targeted for various cancers, with EPZ-6438 as the most advanced (in phase I or II clinical trials for non-Hodgkin's lymphoma, B-cell lymphoma, synovial sarcoma, renal, soft tissue sarcoma, breast and mesothelioma cancers) among all currently active cancer drug programs [55, 57]. Here, EZH2 is linked to cancer.