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HMTi 2017-05-19T11:28:30+00:00

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 targets Clinical trials**
EPZ-5676 DOT1L (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-01294 G9A (EHMT2, KMT1C), GLP (EHMT1, KMT1D)
BIX-01338 SUV39H1 (KMT1A), SUV39H2 (KMT1B)
BRD4770 G9A (EHMT2, KMT1C), GLP (EHMT1, KMT1D)
Chaetocin SUV39H1 (KMT1A), SUV39H2 (KMT1B)
E72 G9A (EHMT2, KMT1C), GLP (EHMT1, KMT1D)
EI1 EZH2 (KMT6A)
EPZ004777 DOT1L (KMT4)
EPZ00568 EZH2 (KMT6A)
EPZ005687 EZH2 (KMT6A)
GSK126 EZH2 (KMT6A)
GSK343 EZH2 (KMT6A)
NC0642 G9A (EHMT2, KMT1C)
SGC0946 DOT1L (KMT4)
UNC0224 G9A (EHMT2, KMT1C), GLP (EHMT1, KMT1D)
UNC0321 G9A (EHMT2, KMT1C), GLP (EHMT1, KMT1D)
UNC0638 G9A (EHMT2, KMT1C), GLP (EHMT1, KMT1D)
UNC0965 G9A (EHMT2, KMT1C), GLP (EHMT1, KMT1D)
UNC1999 EZH2 (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)