ABSTRACT Epigenetics plays a crucial role in gene regulation, and its implications in cancer therapy have led to the development of innovative epigenetic drugs. This review explores the fundamental principles of epigenetic modifications and highlights recent advancements in epigenetic pharmacology for cancer treatment and prevention. Current FDA-approved epigenetic therapies primarily include inhibitors targeting DNA methyl transferases (DNMTs) and histone deacetylases (HDACs). However, future therapeutic strategies may involve inhibitors of histone methyltransferases, histone demethylases, and other key epigenetic regulators. Epigenetic drugs exert their effects in two interconnected ways. Firstly, they restore aberrant epigenetic modifications in malignant and premalignant cells, thereby reversing dysregulated gene expression and serving as a foundation for epigenetic therapy. Secondly, these drugs modulate non-histone proteins that regulate crucial cellular processes such as proliferation, migration, and apoptosis. Through these mechanisms, epigenetic drugs induce cancer cell cycle arrest, differentiation, inhibition of tumour angiogenesis, and cell death via apoptosis, autophagy, necrosis, or mitotic catastrophe. This review provides an in-depth analysis of the molecular mechanisms underlying epigenetic drug action and their clinical applications. With ongoing research, novel epigenetic therapies hold promise for more precise and effective cancer treatments, paving the way for personalized medicine in oncology.