Internal medicine

Cancer drugs

Bioinformatics

Biology

Gene

Cancer

Gene expression

Epigenesis

DNA methylation

Drug

Epigenetic therapy

Drug development

Computational biology

Drug discovery

Cancer therapy

Epigenetics

Clinical trial

Genetics

Medicine

Pharmacology

Nature Medicine

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. Targeting epigenetic modifications is an effective cancer therapeutic approach and can be combined with other therapeutics for maximal effect.

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