Journal
LEUKEMIA & LYMPHOMA
Volume 59, Issue 7, Pages 1574-1585Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/10428194.2018.1430795
Keywords
Epigenetic; non-Hodgkin lymphoma; EZH2 inhibitors
Categories
Funding
- National Institutes of Health
- St. Baldrick's Foundation Fellowship [522077]
- Unravel Pediatric Cancer
- NATIONAL CANCER INSTITUTE [K08CA219473] Funding Source: NIH RePORTER
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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.
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