Epigenetics in Breast Cancer Therapy-New Strategies and Future Nanomedicine Perspectives

Verona Buocikova, Ivan Rios-Mondragon, Eleftherios Pilalis, Aristotelis Chatziioannou, Svetlana Miklikova, Michal Mego, Karlis Pajuste, Martins Rucins, Naouale El Yamani, Eleonora Marta Longhin, Arkadij Sobolev, Muriel Freixanet, Victor Puntes, Aiva Plotniece, Maria Dusinska, Mihaela Roxana Cimpan, Alena Gabelova, Bozena Smolkova

Research output: Contribution to journalReview articlepeer-review

23 Citations (Scopus)


Epigenetic dysregulation has been recognized as a critical factor contributing to the development of resistance against standard chemotherapy and to breast cancer progression via epithelial-to-mesenchymal transition. Although the efficacy of the first-generation epigenetic drugs (epi-drugs) in solid tumor management has been disappointing, there is an increasing body of evidence showing that epigenome modulation, in synergy with other therapeutic approaches, could play an important role in cancer treatment, reversing acquired therapy resistance. However, the epigenetic therapy of solid malignancies is not straightforward. The emergence of nanotechnologies applied to medicine has brought new opportunities to advance the targeted delivery of epi-drugs while improving their stability and solubility, and minimizing off-target effects. Furthermore, the omics technologies, as powerful molecular epidemiology screening tools, enable new diagnostic and prognostic epigenetic biomarker identification, allowing for patient stratification and tailored management. In combination with new-generation epi-drugs, nanomedicine can help to overcome low therapeutic efficacy in treatment-resistant tumors. This review provides an overview of ongoing clinical trials focusing on combination therapies employing epi-drugs for breast cancer treatment and summarizes the latest nano-based targeted delivery approaches for epi-drugs. Moreover, it highlights the current limitations and obstacles associated with applying these experimental strategies in the clinics.

Original languageEnglish
Article number3622
Pages (from-to)E3622
Issue number12
Publication statusPublished - 3 Dec 2020
Externally publishedYes


  • breast cancer
  • drug resistance
  • epi-drugs
  • epigenetics
  • nanomedicine
  • targeted delivery
  • Epi-drugs
  • Targeted delivery
  • Epigenetics
  • Breast cancer
  • Drug resistance
  • Nanomedicine

Field of Science*

  • 3.1 Basic medicine

Publication Type*

  • 1.1. Scientific article indexed in Web of Science and/or Scopus database


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