Welcome to the Cancer Epigenetics Drug database for histone (or lysine) methyltransferase inhibitors. Here you will find drugs that have been approved by the US Food and Drug Administration (FDA) for the treatment of cancers, and/or the clinical trials in which they have or are being tested. Clinical trials are either Phase I (enroll about 15-30 cancer patients to test if the new treatment is safe, to investigate the best way to administer the experimental drugs, and whether cancer is responding to the treatment), Phase II (enroll 100 or less patients to test if the new drug works against a cancer, and to monitor side effects in a group of patients larger than in Phase I), Phase III (enroll hundreds to thousands of patients that are double-blindly assigned either to the experimental or standard treatment to test if the new treatment is better than a standard treatment protocol), or Phase IV (to gather more information about the long-term benefits and side effects of the new drug after it has been FDA-approved). Details on the clinical trials and whether they are ongoing, closed or terminated, and whether results have been posted can be found in the provided links.

Drug*Drug targetsClinical trials**
EPZ-5676DOT1L (KMT4) ALL (I: NCT01684150), AML (I: NCT01684150), MDS (I: NCT01684150)
EPZ-6438 (Tazemetostat)EZH2 (KMT6A)Advanced solid tumors (I: NCT01897571), lymphoma (I: NCT01897571), synovial sarcoma (II: NCT02601950), malignant rhabdoid tumors (II: NCT02601950), rhabdoid tumors of the kidney (II: NCT02601950), atypical teratoid rhabdoid tumors (II: NCT02601950), INI1-negative tumors (II: NCT02601950), malignant rhabdoid tumor of the ovary (II: NCT02601950)
BIX-01294G9A (EHMT2, KMT1C), GLP (EHMT1, KMT1D)
BIX-01338SUV39H1 (KMT1A), SUV39H2 (KMT1B)
BRD4770G9A (EHMT2, KMT1C), GLP (EHMT1, KMT1D)
ChaetocinSUV39H1 (KMT1A), SUV39H2 (KMT1B)
E72G9A (EHMT2, KMT1C), GLP (EHMT1, KMT1D)
EI1EZH2 (KMT6A)
EPZ004777DOT1L (KMT4)
EPZ00568EZH2 (KMT6A)
EPZ005687EZH2 (KMT6A)
GSK126EZH2 (KMT6A)
GSK343EZH2 (KMT6A)
NC0642G9A (EHMT2, KMT1C)
SGC0946DOT1L (KMT4)
UNC0224G9A (EHMT2, KMT1C), GLP (EHMT1, KMT1D)
UNC0321G9A (EHMT2, KMT1C), GLP (EHMT1, KMT1D)
UNC0638G9A (EHMT2, KMT1C), GLP (EHMT1, KMT1D)
UNC0965G9A (EHMT2, KMT1C), GLP (EHMT1, KMT1D)
UNC1999EZH2 (KMT6A)

© CEDD v0.1, Cancer Epigenetics Society, B² Scientific Group, Ltd

*This database is continuously expanding and is weekly updated; please check periodically. Please feel free to write to us at info@ces.b2sg.org under the Subject line: CEDD suggestion, with any suggestion of additional drugs, or to report new epigenetic targets, clinical trials, or FDA-approved cancer applications.

**Abbreviations: ALL: Acute Lymphocytic Leukemia; MDS: Myelodysplastic Syndrome; MLL: Myeloid Lymphocytic Leukemia. Roman numbers between brackets denote Phase I, II, or III clinical trials.

To cite this database: M. Licheva & I.M. Bennani-Baiti. Histone methyltransferase inhibitors, Cancer Epigenetics Drug Database (CEDD) v0.1, Cancer Epigenetics Society (http://ces.b2sg.org/cedd/hmti/), 2016.

  • EPZ-5676_Cancer Epigenetics Society (CES)
  • EPZ-6438_Cancer Epigenetics Society (CES)
  • BIX-01294_Cancer Epigenetics Society (CES)