Current Oncology Reports

, 21:13 | Cite as

BET and EZH2 Inhibitors: Novel Approaches for Targeting Cancer

  • Sofia Genta
  • Maria Cristina Pirosa
  • Anastasios StathisEmail author
Evolving Therapies (RM Bukowski, Section Editor)
Part of the following topical collections:
  1. Topical Collection on Evolving Therapies


Purpose of Review

Increasing evidence suggests that epigenome plays a central role in cancer development making it a promising target for anticancer treatments. Here, we review two new classes of epigenome-targeting agents: the bromodomain and extraterminal domain proteins (BET) inhibitors and the enhancer of zeste homolog (EZH2) inhibitors.

Recent Findings

Clinical research evaluating BET and EZH2 inhibitors is still at an early stage; however, both classes of drugs have demonstrated activity among different hematologic malignancies and solid tumors.


Several studies on BETi and EZH2i are ongoing to better define their potential role in cancer treatment, which patients are most likely to benefit and if the association with other drugs can improve their efficacy.


Bromodomain and extraterminal motif proteins inhibitor (BETi) Enhancer of zeste homolog 2 inhibitor (EZH2i) Epigenetic agents Hematological malignancies Solid tumors 


Compliance With Ethics Guidelines

Conflict of Interest

Sofia Genta declares that she has no conflict of interest.

Maria Cristina Pirosa declares that she has no conflict of interest.

Anastasios Stathis has received research funding (paid to his institution) from Amgen, Bayer, Novartis, Pfizer, Roche, and MEI Pharma, and has received travel grants from AbbVie and PharmaMar.

Human and Animal Rights and Informed Consent

This article does not contain any studies with human or animal subjects performed by any of the authors.


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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2019

Authors and Affiliations

  • Sofia Genta
    • 1
  • Maria Cristina Pirosa
    • 1
  • Anastasios Stathis
    • 1
    Email author
  1. 1.Medical OncologyOncology Institute of Southern SwitzerlandBellinzonaSwitzerland

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