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 |
| Â | BET inhibitor | None | INCB057643, BMS-986158, JAB-8263 |
| Â | EZH2 inhibitor | Tazemetostat (advanced epithelioid sarcoma/follicular lymphoma) | CPI-1205, PF-06821497, SHR2554, CPI-0209 |
| Â | KDM1A inhibitor | None | Seclidemstat, IMG-7289, GSK2879552, INCB059872 |