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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.