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. Author manuscript; available in PMC: 2021 Jul 1.
Published in final edited form as: Trends Cancer. 2020 Mar 31;6(7):580–592. doi: 10.1016/j.trecan.2020.02.003

Table 2.

Epigenetic Drugs Approved or under Clinical Trials

Category Target Approved drug and indications Drugs under clinical trials
DNMT inhibitor DNA methylation writers Azacitidine (myelodysplastic syndromes), decitabine (myelodysplastic syndromes), procainamide (cardiac arrhythmias), hydralazine (essential hypertension), procaine (local anesthetics) Tioguanine, FdCyd, TdCyd, Aza-TdCyd, fluorocyclopentenylcytosine, guadecitabine
HDAC inhibitor Histone acetylation erasers Vorinostat (cutaneous T cell lymphoma), romidepsin (cutaneous T cell lymphoma), belinostat (peripheral T cell lymphoma), panobinostat (multiple myeloma), valproic acid (seizures), chidamide (peripheral T-cell lymphoma, by CFDA) Tacedinaline, mocetinostat, abexinostat, entinostat, pracinostat, resminostat, givinostat, quisinostat, kevetrin, tefinostat, nanatinostat, domatinostat, ricolinostat, ME-344, CG200745, CUDC-101, AR42
KMT6A inhibitor Histone methylation writer Tazemetostat (epithelioid sarcoma) SHR2554, CPI-1205, GSK2816126, PF-06821497, MAK683
SIRT activator Histone acetylation erasers None SRT2104
BET inhibitor Histone acetylation readers None Mivebresib, molibresib, birabresib, INCB057643, ZEN003694, FT-1101, GSK2820151, CC-90010, CPI-0610, PLX51107, ABBV-744, BAY1238097, BI 894999, BMS-986158, GS-5829
PRMT5 inhibitor Histone methylation writer None JNJ-64619178, PF-06939999, GSK3326595
PRMT1 inhibitor Histone methylation writer None GSK3368715
KDM1A inhibitor Histone methylation eraser None Seclidemstat, IMG-7289, tranylcypromine, GSK2879552, INCB059872, phenelzine sulfate
KMT4 inhibitor Histone methylation writer None Pinometostat