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Peer-reviewedCC BY 4.0Frontiers in Pharmacology

Pharmacoepigenetics: from epigenetic regulation to personalized therapeutics

  1. 1Paul L. Foster School of Medicine, Texas Tech University

Abstract

Pharmacoepigenetics is an emerging field of precision medicine that examines how epigenetic modifications influence interindividual variability in drug response. This review discusses the clinical utility of epigenetic therapy in personalized medicine. Current FDA-approved epigenetic drugs including DNA methyltransferase inhibitors, histone deacetylase inhibitors, EZH2 inhibitors, mutant IDH inhibitors, and menin inhibitors are reviewed along with emerging therapies such as BET inhibitors, LSD1 inhibitors, precision epigenetic editing, and combination treatment strategies. Despite notable advances, challenges such as target selectivity, dose-limiting toxicity, epigenetic variability and lack of biomarkers for predicting response or selecting patients continue to limit broader clinical implementation of epigenetic drugs. Continued progress is expected to expand the role of pharmacoepigenetics and improve treatment across a growing range of diseases other than oncology.

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BibTeX
@article{nguyen2026pharmacoepigenetics,
  title = {{Pharmacoepigenetics: from epigenetic regulation to personalized therapeutics}},
  author = {Ashley M. Nguyen and Tamer E. Fandy},
  journal = {Frontiers in Pharmacology},
  year = {2026},
  month = oct,
  doi = {10.3389/fphar.2026.1965981},
  url = {https://www.frontiersin.org/articles/10.3389/fphar.2026.1965981/full},
  note = {CC BY 4.0},
}
RIS
TY  - JOUR
TI  - Pharmacoepigenetics: from epigenetic regulation to personalized therapeutics
AU  - Ashley M. Nguyen
AU  - Tamer E. Fandy
PY  - 2026
DA  - 2026/10/16
JO  - Frontiers in Pharmacology
DO  - 10.3389/fphar.2026.1965981
UR  - https://www.frontiersin.org/articles/10.3389/fphar.2026.1965981/full
AB  - Pharmacoepigenetics is an emerging field of precision medicine that examines how epigenetic modifications influence interindividual variability in drug response. This review discusses the clinical utility of epigenetic therapy in personalized medicine. Current FDA-approved epigenetic drugs including DNA methyltransferase inhibitors, histone deacetylase inhibitors, EZH2 inhibitors, mutant IDH inhibitors, and menin inhibitors are reviewed along with emerging therapies such as BET inhibitors, LSD1 inhibitors, precision epigenetic editing, and combination treatment strategies. Despite notable advances, challenges such as target selectivity, dose-limiting toxicity, epigenetic variability and lack of biomarkers for predicting response or selecting patients continue to limit broader clinical implementation of epigenetic drugs. Continued progress is expected to expand the role of pharmacoepigenetics and improve treatment across a growing range of diseases other than oncology.
SN  - 1663-9812
ER  -