A hypomethylating agent (or demethylating agent[1]) is a drug that inhibits DNA methylation: the modification of DNA nucleotides by addition of a methyl group. Because DNA methylation affects cellular function through successive generations of cells without changing the underlying DNA sequence, treatment with a hypomethylating agent is considered a type of epigenetic therapy.
Currently available hypomethylating agents block the activity of DNA methyltransferase (DNA methyltransferase inhibitors / DNMT inhibitors).
Currently two members of the class, azacitidine and decitabine, are FDA-approved for use in the United States in myelodysplastic syndrome and are being investigated for use in a number of tumors.[2]
^Garcia-Manero G (November 2008). "Demethylating agents in myeloid malignancies". Curr Opin Oncol. 20 (6): 705–10. doi:10.1097/CCO.0b013e328313699c. PMC 3873866. PMID 18841054.
^Hambach L, Ling KW, Pool J, et al. (December 2008). "Hypomethylating drugs convert HA-1 negative solid tumors into targets for stem cell based immunotherapy". Blood. 113 (12): 2715–22. doi:10.1182/blood-2008-05-158956. PMID 19096014.
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