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BET and EZH2 Inhibitors: Novel Approaches for Targeting Cancer

Sofia Genta1, Maria Cristina Pirosa1, Anastasios Stathis2

  • 1Medical Oncology, Oncology Institute of Southern Switzerland, Ospedale San Giovanni, 6500, Bellinzona, Switzerland.

Current Oncology Reports
|February 5, 2019
PubMed
Abstract

Insights

Epigenome-targeting drugs, including bromodomain and extraterminal domain (BET) and enhancer of zeste homolog (EZH2) inhibitors, show promise in cancer treatment. Ongoing research aims to optimize their use in hematologic malignancies and solid tumors.

Area of Science:

  • Oncology
  • Epigenetics
  • Pharmacology

Background:

  • The epigenome is increasingly recognized for its crucial role in cancer development.
  • Epigenetic modifications offer promising therapeutic targets for novel anticancer strategies.

Purpose of the Study:

  • To review two emerging classes of epigenome-targeting agents: bromodomain and extraterminal domain (BET) inhibitors and enhancer of zeste homolog (EZH2) inhibitors.
  • To summarize the current clinical research status and potential applications of these agents in cancer therapy.

Main Methods:

  • Review of current clinical research and preclinical data on BET and EZH2 inhibitors.
  • Analysis of demonstrated activity in various hematologic malignancies and solid tumors.

Main Results:

  • Early-stage clinical research indicates that both BET and EZH2 inhibitors exhibit activity across diverse cancer types.
  • Ongoing studies are focused on defining optimal patient populations, treatment efficacy, and combination strategies.

Conclusions:

  • BET and EZH2 inhibitors represent a promising new frontier in epigenome-based cancer therapy.
  • Further clinical investigation is essential to establish their precise role and maximize their therapeutic benefit in oncology.
Keywords:
Bromodomain and extraterminal motif proteins inhibitor (BETi)Enhancer of zeste homolog 2 inhibitor (EZH2i)Epigenetic agentsHematological malignanciesSolid tumors

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