Enhancer of zeste homolog 2 (EZH2) inhibitors

Dysregulation from the histone methyltransferase EZH2 plays a vital role in the introduction of a number of malignancies including B-cell lymphomas. Consequently, a number of small molecule inhibitors of EZH2 happen to be developed and studied within the pre-clinical setting. Three EZH2 inhibitors: tazemetostat (EPZ-6438), GSK2816126 and CPI-1205 have moved into phase I/phase II numerous studies in patients with non-Hodgkin lymphoma and genetically defined solid tumors. Early data in the tazemetostat trials indicate a suitable safety profile and early indications of activity in diffuse large B-cell lymphoma and follicular lymphoma, including patients with EZH2 wild-type and mutant tumors. Within this review, we present the explanation, key pre-clinical and early clinical findings of small molecule EZH2 inhibitors to be used in lymphoma in addition to Lirametostat future challenges and potential possibilities for combination therapies.