EZH2 inhibitors block the methyltransferase activity of PRC2, reducing H3K27 trimethylation and derepressing genes involved in antigen presentation and differentiation; combination with checkpoint inhibition is under evaluation (e.g., tazemetostat plus pembrolizumab in advanced urothelial carcinoma) [47,48]. The gene discussed is EZH2; the disease is urothelial carcinoma.