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Targeting key epigenetic regulators in solid tumors: focus on EZH2, PRMT5, and BET inhibitors

Irene Hernández de Córdoba Sánchez1, Mercedes Avedillo Ruidiaz2, Victor Moreno3

  • 1Department of Medical Oncology, University Hospital Infanta Sofía, San Sebastián de los Reyes, 28702 Madrid, Spain.

Cancer Treatment Reviews
|May 7, 2026
PubMed

Insights

Epigenetic inhibitors targeting EZH2, PRMT5, and BET proteins show promise for solid tumors. Advances include clinical approval for EZH2 inhibitors and novel strategies for PRMT5 and BET inhibitors in precision oncology.

Area of Science:

  • Oncology
  • Epigenetics
  • Molecular Biology

Background:

  • Epigenetic dysregulation is a key feature of cancer.
  • Epigenetic regulators are emerging as critical therapeutic targets in solid tumors.

Purpose of the Study:

  • To review recent advances in targeting epigenetic regulators EZH2, PRMT5, and BET proteins for solid tumor treatment.
  • To analyze ongoing investigations and future directions for epigenetic therapies in oncology.

Main Methods:

  • Literature review of key advances in epigenetic drug development.
  • Analysis of clinical trial data and preclinical studies for EZH2, PRMT5, and BET inhibitors.
  • Examination of biomarker-driven strategies and combination therapies.

Main Results:

  • EZH2 inhibition gained clinical approval for epithelioid sarcoma.
  • PRMT5 inhibitors demonstrate biomarker-driven synthetic lethality in MTAP-deleted tumors.
  • BET inhibitors show potential in combination therapies despite monotherapy challenges.

Conclusions:

  • Epigenetic inhibitors represent a growing area of precision oncology.
  • Targeting epigenetic regulators offers a promising approach to bridge chromatin biology and clinical benefit in solid tumors.
Keywords:
BET inhibitorsChromatin remodelingEZH2 inhibitorsEpigenetic therapyPRMT5 inhibitorsSolid tumors

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