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. 2021 Jan 26;23:1136–1160. doi: 10.1016/j.omtn.2021.01.024

Table 3.

Drugs that target epigenetic regulation that have been approved or are in clinical trials

Drug Epigenetic mechanisms Phase Disease Reference or ClinicalTrials.gov identifier
Azacitidine DNMTi FDA approved MDS 216
Guadecitabine DNMTi III AML NCT02920008
Entinostat HDACi III breast adenocarcinoma NCT02115282
Vorinostat HDACi FDA approved CTCL 217
Romidepsin HDACi FDA approved CTCL 216
Panobinostat HDACi FDA approved multiple myeloma 218
Givinostat HDACi II chronic myeloproliferative neoplasms NCT01761968
Mocetinostat HDACi II non-small cell lung cancer NCT02954991
Valproic acid HDACi I CLL NCT00810680
Belinostat HDACi FDA approved PTCL 219
CXD101 HDACi I advanced cancer NCT01977638
MPT0E028 HDACi I advanced solid malignancies NCT02350868
CPI-1205 EZH2 inhibitor I B cell lymphoma NCT02395601
Tazemetostat EZH2 inhibitor II diffuse large B cell lymphoma NCT02875548

DNMTi, DNA methyltransferases inhibitor; FDA, US Food and Drug Administration; MDS, myelodysplastic syndrome; AML, acute myeloid leukemia; HDACi, histone deacetylases inhibitor; CTCL, cutaneous T cell lymphoma; CLL, chronic lymphocytic leukemia; PTCL, peripheral T cell lymphoma; EZH2, enhancer of zeste 2.