The incidence of cancer is sharply rising worldwide. Numerous factors like poor clinical outcomes, drug resistance, restricted treatment options, and delayed diagnosis are to blame for the higher incidence rate. Recent research indicates that epigenetic modifications are necessary in the etiology of cancer. Modifications to noncoding RNA, histones, and DNA methylation influence cancer. In epigenetic drug discovery, notable progress has been made recently. Additionally, the development of nanotechnologies in medicine has opened up new avenues for increasing epi-drugs’ effectiveness by targeting drug delivery, their stability and solubility, and reducing side effects. Effective molecular epidemiological screening techniques and omics technologies enable patient classification and tailored management of emerging diagnostic and prognostic epigenetic biomarkers. This chapter aims to clarify and explore the current status of epigenetics in the initiation and progression of cancer, as well as how epigenetic therapy—often used along with other therapies—will soon prove to be an effective instrument for managing cancer.