Table 2.

Epigenetic-based therapeutics in preclinical and clinical development

Epigenetic targetCompoundDevelopmental stageReferences
HDACs (class I, IIa, IIb, IV)Vorinostat (SAHA)FDA approved for CTCL49, 104, 113
Panobinostat (LBH589)Phase I/II
Belinostat (PXD101)Phase I/II
ITF2357Phase I
PCI-24781Phase I
HDACs (class I, IIa)PhenylbutyratePhase I/II49, 104, 113
VPAPhase I/II
HDACS 1, 2Romidepsin (depsipeptide)Phase I/II49, 104, 113
SK-7041Experimental
SK-7068Experimental
HDACs 1, 3MS-275Phase I/II49, 104, 113
CI-994Phase I
MGCD0103Phase I/II
HDACs 2, 3ApicidinExperimental49, 104, 113
HDAC 6TubacinExperimental49, 104, 113
HDAC8SB-379872AExperimental49, 104, 113
PCI-34051Experimental
DNMTVidaza (5-azacytidine)FDA approved for myelodysplatic syndromes86, 114–116
Decitabine (5-aza-2′-deoxycytidine)
ZebularineExperimental
RG108Experimental
ProcaineExperimental
HydralazinePhase I
(-)-epigallocatechin-3-gallate noncovalent enzyme (EGCG)Experimental
SIRT1-7NicotinamideExperimental93
SIRT1, 2Tenovin-1-3, 5-6Experimental92
SirtinolExperimental93
SplitomycinExperimental117
CambinolExperimental
SIRT1SRT1720Experimental78, 118
EX-527Experimental
NF657
SIRT2AGK2Experimental119
SIRT5SuraminExperimental93
HMT (G9a)BIX-01294Experimental96
HMT (SU(VAR)3-9, G9a)ChaetocinExperimental94
Polycomb group proteinsDZNepExperimental97
LSD1Polyamine analogsExperimental98

Abbreviation: CTCL, cutaneous T-cell lymphoma.