Tazemetostat: a treatment option for relapsed/refractory follicular lymphoma.

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.

• Authors: Patrizia Mondello, Stephen M Ansell
• Journal: Expert opinion on pharmacotherapy (Expert Opin Pharmacother) Vol. 23 Issue 3 Pg. 295-301 (Feb 2022) ISSN: 1744-7666 [Electronic] England
• PMID: 34904909 (Publication Type: Journal Article)

Chemical References

• Benzamides
• Biphenyl Compounds
• Morpholines
• Pyridones
• Enhancer of Zeste Homolog 2 Protein
• tazemetostat

Topics

• Benzamides
• Biphenyl Compounds
• Enhancer of Zeste Homolog 2 Protein (genetics)
• Humans
• Lymphoma, Follicular (drug therapy, genetics)
• Morpholines
• Pyridones