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 |
| PMCID: | PMC6659997 |
| DOI/URL: | |
| Notes: | Review -- Export Date: 1 August 2018 -- Source: Scopus |
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