Enhancer of zeste homolog 2 (EZH2) inhibitors Journal Article


Authors: Gulati, N.; Béguelin, W.; Giulino-Roth, L.
Article Title: Enhancer of zeste homolog 2 (EZH2) inhibitors
Abstract: Dysregulation of the histone methyltransferase EZH2 plays a critical role in the development of a variety of malignancies including B-cell lymphomas. As a result, a series of small molecule inhibitors of EZH2 have been developed and studied in the pre-clinical setting. Three EZH2 inhibitors: tazemetostat (EPZ-6438), GSK2816126 and CPI-1205 have moved into phase I/phase II clinical trials in patients with non-Hodgkin lymphoma and genetically defined solid tumors. Early data from the tazemetostat trials indicate an acceptable safety profile and early signs of activity in diffuse large B-cell lymphoma and follicular lymphoma, including patients with EZH2 wild-type and mutant tumors. In this review, we present the rationale, key pre-clinical and early clinical findings of small molecule EZH2 inhibitors for use in lymphoma as well as future challenges and potential opportunities for combination therapies. © 2018, © 2018 Informa UK Limited, trading as Taylor & Francis Group.
Keywords: unclassified drug; review; cancer patient; antineoplastic agent; b lymphocyte; drug mechanism; lymphoma; drug use; non-hodgkin lymphoma; epigenetic; clinical trial (topic); transcription factor ezh2; methyltransferase inhibitor; human; priority journal; tazemetostat; ezh2 inhibitors; cpi 1205; gsk 2816126
Journal Title: Leukemia and Lymphoma
Volume: 59
Issue: 7
ISSN: 1042-8194
Publisher: Taylor & Francis Group  
Date Published: 2018-01-01
Start Page: 1574
End Page: 1585
Language: English
DOI: 10.1080/10428194.2018.1430795
PROVIDER: scopus
PUBMED: 29473431
DOI/URL:
Notes: Review -- Export Date: 1 August 2018 -- Source: Scopus
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MSK Authors
  1. Lisa B Giulino
    15 Giulino
  2. Nitya Gulati
    3 Gulati
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