Clinical Advances in Hypomethylating Agents Targeting Epigenetic Pathways

DNA methylation and histone acetylation are two most studied epigenetic markers. Aberrant methylation of gene promoter regions and histone tail lysine residue modification through acetylation and methylation play a key role in malignant disorders. Two DNA methyltransferase inhibitors, azacitidine and decitabine, have been licensed for clinical therapy for patients with myelodysplastic syndrome. New hypomethylating agents, zebularine and isothiocyanates, are in various stages of development for cancer therapy. In this review we summarize recent clinical developments on novel hypomethylating agents and new regimens from clinical trials for epigenetic therapy of cancer.