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Table 3 Epigenetic clinical trials for aging-related degenerative diseasesa

From: Epigenetic regulation of caloric restriction in aging

Drugs Epigenetic effect Description Clinical trials References
Azacitidine DNMT inhibitors 5-azacytidine; a chemical analogue of cytidine that affects DNA methylation as a false substrate Phases I, II and III: myelodysplastic syndromes such as leukemia [60]
Decitabine DNMT inhibitors 5-aza-2'-deoxycytidine, a chemical analogue of cytidine that affects DNA methylation as a false substrate Phases I, II and III: myelodysplastic syndromes such as leukemia, cervical, and non-small-cell lung cancer [60]
Depsipeptide HDAC inhibitors Cyclic tetrapeptide Phases I and II: hematological tumors such as leukemia and lymphoma [78, 79]
Phenylbutyrate HDAC inhibitors Aliphatic acid Phases I and II: hematological tumors such as leukemia and lymphoma and colorectal cancer [78, 79]
Valproic acid HDAC inhibitors Aliphatic acid Phase I: hematological tumors such as leukemia and lymphoma [78, 79]
Suberoylanilide hydroxamic acid HDAC inhibitors Hydroxamic acid Phases I and II: hematological tumors, such as leukemia and lymphoma, solid tumors [78, 79]
Resveratrol SIRT1 activator A natural compound enriched in grapes and red wine Phase I and II: diabetes, obesity, Alzheimer's disease and cancers [118, 119]
Genistein Inhibitor of both DNMTs and HDACs Active epigenetic diet found in soybean products Preclinical: diabetes and cancer [61, 63, 122, 123]
EGCG Inhibitor of both DNMTs and HDACs Active epigenetic dietary compound enriched in green tea Phase I: diabetes, cardiovascular disease and cancer [61, 62, 124, 125]
Sulforaphane HDAC inhibitor Active epigenetic dietary compound enriched in broccoli sprouts Preclinical [80, 121]
  1. aDNMT, DNA methyltransferase; HDAC, histone deacetylase; SIRT1, Sirtuin (silent mating type information regulation 2 homolog) 1; EGCG, epigallocatechin gallate.