Epidrugs: targeting epigenetic marks in cancer treatment

Epigenetics. 2019 Dec;14(12):1164-1176. doi: 10.1080/15592294.2019.1640546. Epub 2019 Jul 13.


Growing evidence suggests that aberrant epigenetic regulation of gene function is strongly related to the genesis of cancer. Unlike genetic mutations, the ability to reprogram the epigenetic landscape in the cancer epigenome is one of the most promising target therapies in both treatment and reversibility of drug resistance. Epigenetic alterations in cancer development and progression may be the basis for the individual variation in drug response. Thus, this review focuses on the emerging area of pharmaco(epi)genomics, specifically highlighting epigenetic reprogramming during tumorigenesis and how epigenetic markers are targeted as a therapy (epidrugs) and the clinical implications of this for cancer treatment.

Keywords: Epigenetics; cancer; epidrugs; pharmacology; reprogramming; treatment.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Epigenesis, Genetic / drug effects*
  • Epigenomics / methods
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / genetics
  • Pharmacogenetics / methods


  • Antineoplastic Agents

Grants and funding

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES), Programa de Excelência Acadêmica (CAPES-PROEX) and Programa de Apoio à Pós-Graduação (CAPES-PROAP), Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq, Grant number: 437,037/2018-5, CLMF; 440755/2018-2, CP; 439019/2018-4, GPF) and Fundação Cearense de Apoio ao Desenvolvimento Cientí;fico e Tecnológico (FUNCAP, PPSUS PP3-0118-00070.01.00).