Examples of the steadily growing repertoire of epigenetic therapies for a variety of malignancies that are currently being used or tested in clinical trialsa

DrugTargetEpigenetic classDisease(s) treated
AzacitidineDNA methyltransferase (DNMT1)DNA methylationAML
Decitadine guadecitadineDNA methyltransferase (DNMT1)DNA methylationRecurrent fallopian tube carcinoma; recurrent ovarian carcinoma; recurrent primary peritoneal carcinoma; papillary thyroid carcinoma; follicular thyroid carcinoma; non-small-cell lung cancer; colorectal cancer; metastatic pancreatic adenocarcinoma
VorinostatHistone deacetylaseHistone modificationCutaneous T-cell lymphoma; AML; glioma; prostate cancer
EPZ-5676 (pinometostat)DOT1L (a histone methyltransferase)Histone modificationMLL-rearranged leukemia
TranylcypromineLSD1 (a histone demethylase)Histone modificationAML; refractory solid tumors
CPI-0610BET family proteinsHistone readerLymphoma; multiple myeloma; acute leukemias
GSK525762BET family proteinsHistone readerNUT midline carcinoma
TEN-010BET family proteinsHistone readerAML; refractory solid tumors
AG-120Mutant IDH1Metabolic pathwayAML; glioma; cholangiocarcinoma; refractory solid tumors
TazemetostatEZH2 (a histone methyltransferase)Histone modification (direct); chromatin remodeling complexes (indirect)B-cell lymphoma; mesothelioma; synovial sarcoma; rhabdoid tumors; INI1-negative tumors
  • a AML, acute myeloid leukemia.