Tazemetostat: a treatment option for relapsed/refractory follicular lymphoma

Patrizia Mondello, Stephen M. Ansell

Research output: Contribution to journalArticlepeer-review

Abstract

Introduction: Follicular lymphoma (FL) is the second most common form of B cell lymphoma and generally presents as an indolent and relatively slow-growing tumor. However, most FLs are incurable with a shortening of subsequent responses. Therefore, novel and more effective treatments are desperately needed. Tazemetostat is a first-in-class, selective, oral inhibitor of EZH2, a lysine methyltransferase that is mutated in about 25% of FL. Tazemetostat has been recently approved for relapsed/refractory FL after two or more lines of therapy in the presence of an EZH2 mutation or independent of an EZH2 mutation in the absence of other options. Areas covered: Here, the authors provide a review focusing on the molecular mechanisms of EZH2, clinical development of tazemetostat and other EZH2 inhibitors (EZH2i), as single-agent therapy and in combinatorial regimens. Finally, they provide a futuristic look at therapeutic approaches for this disease. Expert opinion: Tazemetostat monotherapy showed clinically meaningful and durable responses with a favorable toxicity profile, especially in EZH2 mutant lymphoma. Future studies should explore mechanism-based combinatorial regimens to maximize and prolong the anti-lymphoma effect.

Original languageEnglish (US)
JournalExpert Opinion on Pharmacotherapy
DOIs
StateAccepted/In press - 2021

Keywords

  • epigenetics
  • EZH2
  • follicular lymphoma
  • precision therapy
  • tazemetostat

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

Fingerprint

Dive into the research topics of 'Tazemetostat: a treatment option for relapsed/refractory follicular lymphoma'. Together they form a unique fingerprint.

Cite this