Cancer is an uncontrolled malignant tumor growth taking place in any tissue of the body and attains complex diversity which makes it difficult for oncologists to choose therapeutics. The changes leading to formation of cancerous cells occur due to a series of molecular events. Now scientists are trying to understand the various molecular processes that are involved in the growth of cancers. This article presents a brief account of epigenetics with reference to DNA methylation and histone modification as an important contributor to the formation of cancer cells. Drug targeting the epigenetic regulators has been considered for various types of cancer. The enzymes in DNA methylation and histone modification, FDA approved clinical drugs along with the challenges associated with the development of anti-cancer target based therapeutics are summarized.