EZH2 and diffuse large B-cell lymphoma: GSK126 is a potent and highly selective EZH2 inhibitor that targets both wild-type EZH2 and Y641 mutant EZH2.1346 However, a phase I clinical trial assessing its safety, pharmacokinetics, pharmacodynamics, and clinical activity in patients with relapsed or refractory DLBCL, other NHLs, multiple myeloma, and solid tumors was terminated.