This book covers the development and therapeutic applications of epigenetic inhibitors. The last decade has seen an explosion of technologies that can track, assemble, and decode the complexity of the cell at a level never attained before. These new technologies allowed the detection, mapping, and modification of the “epigenetic code” to uncover the drastic roles that epigenetics play in the etiology of human diseases. The recent development of novel inhibitors against some of these epigenetic modifiers started a race to further characterize the biology of these regulators, and understand their roles in various diseases. Much remains to be discovered, and this book summarizes what has been accomplished and looks towards the future of epigenomics in medicine.