Table 1 Epigenetic drugs approved or under clinical trials

From: Epigenetic regulation in the tumor microenvironment: molecular mechanisms and therapeutic targets

Epigenetic targeting

Category

Approved drugs and conditions

Drugs under clinical trials

DNA methylation

DNMT inhibitor

Azacitidine (juvenile myelomonocytic leukemia/acute myeloid leukemia), Decitabine (myelodysplastic syndromes)

Guadecitabine, Tioguanine, FdCyd, TdCyd, aza-TdC, RX-3117, NTX-301

Histone modification

HDAC inhibitor

None

Vorinostat, Romidepsin, Panobinostat, Belinostat, Valproic acid, Chidamide, Mocetinostat, Entinostat, Abexinostat, Domatinostat, Tinostamustine, ACY-241, KA-2507, AR-42, Nanatinostat, ITF2357, SB939, Resminostat, ACY-1215

 

BET inhibitor

None

INCB057643, BMS-986158, JAB-8263

 

EZH2 inhibitor

Tazemetostat (advanced epithelioid sarcoma/follicular lymphoma)

CPI-1205, PF-06821497, SHR2554, CPI-0209

 

KDM1A inhibitor

None

Seclidemstat, IMG-7289, GSK2879552, INCB059872