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. 2014 Sep 5;172(11):2716–2732. doi: 10.1111/bph.12844

Table 2.

Inhibitors of epigenetic erasers

Category Compound Phase Tumour type References
Histone demethylase inhibitors
 LSD1 inhibitors Tranylcypromine Preclinical AML Schenk et al., 2012
ORY-1001 Clinical trials Relapsed or refractory acute leukaemia 2013-002447-29
 JMJC domain-containing inhibitors 8-hydroxyquinolines Preclinical (Enzymatic inhibition of the target protein) King et al., 2010
Pyridine hydrazones Preclinical (Enzymatic inhibition of the target protein) Chang et al., 2011
GSK-J1 Preclinical (Enzymatic inhibition of the target protein) Kruidenier et al., 2012
HDAC inhibitors
 Cyclic peptides Romidepsin Approved Refractory cutaneous T-cell lymphoma Whittaker et al., 2010
 Hydroxamic acids TCA Preclinical Lung Chan et al., 2013
Vorinostat Approved Cutaneous T-cell lymphoma, lymphoid malignancies Mann et al., 2007; NCT00691210
Panobinostat Clinical trials Haematological malignancies, solid tumours Cassier et al., 2014; NCT01321346
Belinostat Clinical trials Ovary, colon, haematological malignancies Plumb et al., 2003; NCT01686165
Pracinostat Clinical trials Colorectal, MDS Novotny-Diermayr et al., 2010; NCT01873703
Quisinostat Clinical trials Advanced solid tumours, cutaneous T-cell lymphoma Venugopal et al., 2013; NCT01486277
CHR-3996 Clinical trials Refractory solid tumours Banerji et al., 2012; NCT00697879
 Short-chain fatty acids Phenylacetate Clinical trials Brain NCT00003241
Phenylbutirate Clinical trials Advanced colorectal cancer NCT00002796
Valproic acid Clinical trials Leukaemia, solid tumours Fredly et al., 2013; Coronel et al., 2011
 Benzamides Entinostat Clinical trials Refractory advanced non-small cell lung cancer Juergens et al., 2011
Mocetinostat Clinical trials Haematological malignancies, advanced solid tumours Younes et al., 2011; Siu et al., 2008
CS055 Clinical trials Advanced non-small cell lung cancer NCT01836679