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Targeting epigenetic modifications in cancer therapy: erasing the roadmap to cancer

Nature Medicine volume 25, pages 403–418 (2019)Cite this article

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Abstract

Epigenetic dysregulation is a common feature of most cancers, often occurring directly through alteration of epigenetic machinery. Over the last several years, a new generation of drugs directed at epigenetic modulators have entered clinical development, and results from these trials are now being disclosed. Unlike first-generation epigenetic therapies, these new agents are selective, and many are targeted to proteins which are mutated or translocated in cancer. This review will provide a summary of the epigenetic modulatory agents currently in clinical development and discuss the opportunities and challenges in their development. As these drugs advance in the clinic, drug discovery has continued with a focus on both novel and existing epigenetic targets. We will provide an overview of these efforts and the strategies being employed.

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Fig. 1: Immuno-oncology mechanisms targeted by epigenetic therapies in the clinic.
Fig. 2: Strategies for combining epigenetic modulatory drugs.

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  1. Epigenetics Department, Oncology, GlaxoSmithKline, Collegeville, PA, USA

    Helai P. Mohammad, Olena Barbash & Caretha L. Creasy

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Mohammad, H.P., Barbash, O. & Creasy, C.L. Targeting epigenetic modifications in cancer therapy: erasing the roadmap to cancer. Nat Med 25, 403–418 (2019). https://doi.org/10.1038/s41591-019-0376-8

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