Rewriting heart health: epigenetic drugs in cardiovascular medicine
Abstract
Cardiovascular disease reflects not only genetic pre-disposition and haemodynamic stress but also reversible alterations in chromatin organization and transcriptional programming, a layer of regulation that is, in principle, amenable to pharmacological intervention. Purpose-built epigenetic drugs, DNA methyltransferase inhibitors, histone deacetylase inhibitors, histone acetyltransferase inhibitors, bromodomain and extra-terminal domain inhibitors, enhancer of zeste homolog 2 inhibitors, and RNA-based therapeutics, target this machinery directly. In parallel, established cardiovascular therapies, including statins, renin–angiotensin–aldosterone system inhibitors, beta-blockers, mineralocorticoid receptor antagonists, antithrombotic agents, sodium–glucose cotransporter-2 inhibitors, and incretin-based therapies, appear to modulate the epigenome as an underappreciated component of their action, a concept termed ‘pharmaco-epigenetics’. This review appraises both axes side by side, with explicit attention to clinical maturity, including the level of evidence, human validation, development stage, and the interpretation of hypothesis-generating findings. Key translational barriers, cardiac-targeted delivery, biomarkers of target engagement, and interindividual epigenetic variability, are outlined alongside priorities for future trial design.
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BibTeX
@article{atzemian2026rewriting,
title = {{Rewriting heart health: epigenetic drugs in cardiovascular medicine}},
author = {Natalia Atzemian and Ludovica Di Venanzio and Shafeeq Ahmed Mohammed and Sarah Costantino and Frank Ruschitzka and Francesco Paneni},
journal = {European Heart Journal. Cardiovascular Pharmacotherapy},
year = {2026},
month = sep,
doi = {10.1093/ehjcvp/pvag075},
url = {https://doi.org/10.1093/ehjcvp/pvag075},
note = {CC BY-NC 4.0},
}
RIS
TY - JOUR
TI - Rewriting heart health: epigenetic drugs in cardiovascular medicine
AU - Natalia Atzemian
AU - Ludovica Di Venanzio
AU - Shafeeq Ahmed Mohammed
AU - Sarah Costantino
AU - Frank Ruschitzka
AU - Francesco Paneni
PY - 2026
DA - 2026/09/24
JO - European Heart Journal. Cardiovascular Pharmacotherapy
DO - 10.1093/ehjcvp/pvag075
UR - https://doi.org/10.1093/ehjcvp/pvag075
AB - Cardiovascular disease reflects not only genetic pre-disposition and haemodynamic stress but also reversible alterations in chromatin organization and transcriptional programming, a layer of regulation that is, in principle, amenable to pharmacological intervention. Purpose-built epigenetic drugs, DNA methyltransferase inhibitors, histone deacetylase inhibitors, histone acetyltransferase inhibitors, bromodomain and extra-terminal domain inhibitors, enhancer of zeste homolog 2 inhibitors, and RNA-based therapeutics, target this machinery directly. In parallel, established cardiovascular therapies, including statins, renin–angiotensin–aldosterone system inhibitors, beta-blockers, mineralocorticoid receptor antagonists, antithrombotic agents, sodium–glucose cotransporter-2 inhibitors, and incretin-based therapies, appear to modulate the epigenome as an underappreciated component of their action, a concept termed ‘pharmaco-epigenetics’. This review appraises both axes side by side, with explicit attention to clinical maturity, including the level of evidence, human validation, development stage, and the interpretation of hypothesis-generating findings. Key translational barriers, cardiac-targeted delivery, biomarkers of target engagement, and interindividual epigenetic variability, are outlined alongside priorities for future trial design.
SN - 2055-6837
SN - 2055-6845
ER -