HMT inhibitors 2017-06-03T14:06:49+00:00

To cite this dataset: M. Licheva, A. Neudolt, and I.M. Bennani-Baiti. Clinical trials of histone methyltransferase inhibitors in cancer. Cancer Epigenetics Drug Database (CEDD) – Clinical data, v1.1. Cancer Epigenetics Society (https://ces.b2sg.org/cedd/clinical_kdmi/), 2016.

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 0 (enroll a maximum of 15 patients or healthy volunteers who are administered a single sub-therapeutic dose to study the pharmacokinetics and tumor targeting of the drug), 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 drug, and whether cancer is responding to the treatment), Phase II (enroll 100 or less patients to test if the new drug is effective 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 below.


Drug* Drug targets Clinical trials**
EPZ-5676 DOT1L (KMT4) ALL (I: NCT01684150NCT02141828), AML (I: NCT01684150NCT02141828), leukemia (I: NCT02141828), MDS (I: NCT01684150)
EPZ-6438 (Tazemetostat) EZH2 (KMT6A) Advanced solid tumors (I: NCT01897571), atypical teratoid rhabdoid tumors (II: NCT02601950), B-cell lymphoma (I: NCT01897571), DLBCL (II: NCT01897571), epithelioid sarcoma (II: NCT02601950), follicular lymphoma (II: NCT01897571), INI1-negative tumors (II: NCT02601950), malignant mesothelioma (II: NCT02860286), malignant rhabdoid tumors (II: NCT02601950), malignant rhabdoid tumor of the ovary (II: NCT02601950), renal medullary carcinoma (II: NCT02601950), rhabdoid tumor (I: NCT02601937), rhabdoid tumors of the kidney (II: NCT02601950), synovial sarcoma (I: NCT02601937; II: NCT02601950).

© CEDD v1.1, Cancer Epigenetics Society & B² Scientific Group, Ltd. All rights reserved, 2016.

*This database is continuously expanding and 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; DLBCL: Diffuse large B-cell lymphoma; MDS: Myelodysplastic Syndrome; MLL: Myeloid Lymphocytic Leukemia. Roman numbers between brackets denote Phase I, II, or III clinical trials.

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