Fueled by the vast amount of genomic data generated in many population-scale human sequencing projects, many current research interests and efforts focus on the role of heritable genetic factors in disease and therapy. However, non-genetic factors such as environmental stimuli, age, diseases, diet, lifestyle, and exposure to xenobiotics also contribute substantially to disease susceptibility, etiology, progression, and remission; for example, via epigenetic mechanisms. Accordingly, much research is now devoted to finding epigenetic alterations as diagnostic or prognostic biomarkers to identify at-risk individuals and predict the success of drug therapy. In addition, drugs targeting the epigenetic machinery can increase the success of conventional standard-of-care treatment and are gaining momentum particularly in the area of oncology.