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Enhancer of zeste homolog 2 (EZH2) inhibitors

Nitya Gulati1,2, Wendy Béguelin3, Lisa Giulino-Roth1,2,3

  • 1a Division of Pediatric Hematology/Oncology, Department of Pediatrics , Weill Cornell Medical College , New York , NY , USA.

Leukemia & Lymphoma
|February 24, 2018
PubMed

Insights

Small molecule inhibitors targeting the EZH2 enzyme show promise for treating B-cell lymphomas. Early clinical trials suggest tazemetostat has a good safety profile and activity in diffuse large B-cell lymphoma and follicular lymphoma.

Area of Science:

  • Oncology
  • Epigenetics
  • Pharmacology

Background:

  • Dysregulation of enhancer of zeste homolog 2 (EZH2) is implicated in various cancers, particularly B-cell lymphomas.
  • EZH2 is a histone methyltransferase crucial for epigenetic regulation.

Purpose of the Study:

  • To review the rationale, preclinical, and early clinical findings of small molecule EZH2 inhibitors for lymphoma treatment.
  • To discuss future challenges and opportunities for combination therapies involving EZH2 inhibitors.

Main Methods:

  • Review of preclinical data and early-phase clinical trial results for EZH2 inhibitors.
  • Focus on tazemetostat, GSK2816126, and CPI-1205 in lymphoma and solid tumors.

Main Results:

  • Three EZH2 inhibitors have advanced to Phase I/II clinical trials.
  • Tazemetostat demonstrates an acceptable safety profile and early signs of activity in diffuse large B-cell lymphoma and follicular lymphoma, including wild-type and mutant EZH2 cases.

Conclusions:

  • Small molecule EZH2 inhibitors represent a promising therapeutic strategy for lymphomas.
  • Further research into combination therapies may enhance treatment efficacy.
Keywords:
EZH2 inhibitorsEpigeneticnon-Hodgkin lymphoma

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