The future of epigenetic therapy in solid tumours - Lessons from the past Review uri icon


MeSH Major

  • Antineoplastic Agents
  • Epigenesis, Genetic
  • Genetic Therapy
  • Molecular Targeted Therapy
  • Neoplasms


  • The promise of targeting epigenetic abnormalities for cancer therapy has not been realized for solid tumours, although increasing evidence is demonstrating its worth in haematological malignancies. In fact, true clinical efficacy in haematopoietic-related neoplasms has only become evident at low doses of epigenetic-targeting drugs (namely, inhibitors of histone deacetylase and DNA methyltransferases). Describing data from preclinical studies and early clinical trial results, we hypothesize that in using low-dose epigenetic-modulating agents, tumour cells can be reprogrammed, which overrides any immediate cytotoxic and off-target effect observed at high dose. We suggest that such optimization of drug dosing and scheduling of currently available agents could give these agents a prominent place in cancer management--when used alone or in combination with other therapies. If so, optimal use of these known agents might also pave the way for the introduction of other agents that target the epigenome.

publication date

  • May 2013



  • Review



  • eng

PubMed Central ID

  • PMC3730253

Digital Object Identifier (DOI)

  • 10.1038/nrclinonc.2013.42

PubMed ID

  • 23546521

Additional Document Info

start page

  • 256

end page

  • 66


  • 10


  • 5