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© 2016 Elsevier Inc. All rights reserved. The last decade has brought about a vastly improved understanding of the important role that epigenetic changes play in cancer biology. Epigenetic therapy seeks to harness recent insights into the dynamic nature of the mechanisms involved in epigenetic reprogramming in order to develop new therapeutic modalities for the targeted reversal of some of these epigenetic modifications. Already, six epigenetically acting drugs, two DNA methyltransferase inhibitors, and four histone deacetylase inhibitors, have been approved by the US Food and Drug Administration for the treatment of hematological malignancy. However, not all patients benefit from these drugs. Therefore, the development of biomarkers that allow the identification of patients most likely to benefit from these new treatments is a pressing and as yet unmet medical need. Here we discuss recent advances in the development of epigenetic therapies and associated biomarkers and address how these novel modalities open up new perspectives for the future of cancer management in an era of personalized medicine.

Original publication





Book title

Drug Discovery in Cancer Epigenetics

Publication Date



373 - 406