DNMT inhibitors 2017-06-03T14:10:31+00:00

To cite this dataset: M. Licheva, A. Neudolt, and I.M. Bennani-Baiti. Clinical trials of DNA methyltransferase inhibitors in cancer. Cancer Epigenetics Drug Database (CEDD) – Clinical data, v1.1. Cancer Epigenetics Society (https://ces.b2sg.org/cedd/clinical_dnmti/), 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* Target FDA-approved & Clinical trials**
5-aza-2’-deoxycytidine (Decitabine, Dacogen®, Supergen) DNMT1, DNMT3a, DNMT3b FDA-approved: MDS

Trials: AML (I: NCT01806116, NCT01352650, NCT02412475; II: NCT02785900, NCT02802267, NCT02662647, NCT02472145, NCT02634827NCT02632721; III: NCT02172872), B-cell lymphoma (0: NCT02846935), CML (II: NCT00042003NCT00042016), CMML (II: NCT01251627; NCT01098084; NCT02190695), lung cancer (II: NCT02795923),  MDS (II/III: NCT02744742), MDS (II/III: NCT02850822), metastatic colorectal cancer (I: NCT00879385; I/II: NCT02316028), non-Hodgkin’s lymphoma (0: NCT02846935), NSCLC (I: NCT00084981; I/II: NCT01628471; II: NCT02664181NCT02795923), ovarian cancer (I: NCT01673217; I/II: NCT00477386; II/III: NCT02159820), pancreatic adenocarcinoma (0: NCT02847000), pulmonary metastasis (I: NCT02839694), T-cell lymphoma (0: NCT02846935).

5-azacytidine (Vidaza®) DNMT1 FDA-approved: MDS

Trials: ALL (I: NCT01110473; I/II: NCT02750254), AML (I: NCT02750995, NCT02719574, NCT02782468; I/II: NCT02677922, NCT02829840, NCT02750254; Ib/II: 2014-001345-24; II: NCT02775903NCT00666497, NCT01110473, NCT02450877, 2015-003596-30, NCT02610777; II/III: NCT02752035; III: NCT02785900, NCT02577406), bladder cancer (II: NCT02788201), breast cancer (II: NCT02811497), CLL (I: NCT00079378NCT01110473), CML (I: NCT01110473), CMML (II: NCT01048034, NCT01350947, NCT00946647, NCT02610777), colorectal carcinoma (II: NCT02811497), leukemia (I/II: NCT02829840), malignant skin neoplasms (II: NCT02816021), MDS (I: NCT02750995NCT02719574NCT02782468NCT02783547NCT02721875; I/II: NCT02706899, NCT02750254; Ib/II: 2014-001345-24; II: NCT02775903, NCT02610777, NCT02599649), melanoma (II: NCT02816021), metastatic colorectal cancer (II: NCT02260440; NCT01105377), MM (II: NCT00006019), nasopharyngeal carcinoma (II: NCT02269943), NSCLC (II: NCT01281124NCT01935947), ovarian cancer (II: NCT02811497), SLL (I: NCT00275080), urinary bladder neoplasms (II: NCT02788201), urothelial carcinoma (II: NCT02788201).

5,6-dihydro-5-azacytidine DNMT1 Trials: Lymphoma and ovarian cancer (I: PubMed), melanoma (II: PubMed), NSCLC (II: PubMed), pleural malignant mesothelioma (II: PubMed; PubMed).
5-fluoro-2′-deoxycytidine DNMT1 Trials: Breast cancer (II: NCT00978250).
Curcumin Trials: Adenocarcinoma (II: NCT00094445), advanced cancer (I/II: NCT02138955), CLL (II: NCT02100423), colon cancer (0: NCT02724202), colorectal cancer (I/II: NCT01490996; II: NCT02439385), pancreatic cancer (II: NCT00192842, NCT00094445), prostate cancer (II: NCT02095717NCT02724618).
Disulfiram Trials: Glioblastoma (I: NCT02770378), NSCLC (II/III: NCT00312819), pancreatic cancer (I: NCT02671890), stage IV melanoma (I/II: NCT00256230) . 
Genistein DNMT1, DNMT3a, DNMT3b Trials: Breast cancer (II: NCT00244933NCT00244933), colorectal cancer (I/II: NCT01985763), kidney cancer (I/II: NCT00769990), lymphoma (II: NCT02624388), medulloblastoma (II: NCT02624388), melanoma (I/II: NCT00769990), neuroblastoma (II: NCT02624388), NSCLC (I/II: NCT01628471), prostate cancer (II: NCT01126879, NCT01325311NCT02766478), sarcoma (II: NCT02624388).
Hydralazine DNMT1 Trials: Breast cancer (I/II: NCT00575978; II: NCT00395655), cervical cancer (II: NCT00404326; III: NCT02446652), lung cancer (I: NCT00996060), ovarian cancer (III: NCT00533299), rectal cancer (II: NCT00575640).
S-Equol Trials: Breast cancer (0: NCT02352025).
SGI-110 (MG98)
DNMT1 Trials: AML (I/II: NCT01261312; II:  NCT02096055,  NCT02684162; III: NCT02348489), CMML (I/II: NCT01261312), germ cell tumor (I: NCT02429466), hepatocellular carcinoma (II: NCT01752933), leukemia (II: NCT02684162), MDS (I/II: NCT01261312; II: NCT02684162, NCT02131597NCT02197676), mesothelioma (I: PubMed), metastatic colorectal cancer (I: NCT01966289), metastatic melanoma (I: NCT02608437), ovarian cancer (I/II: NCT01696032), renal cell carcinoma (I: PubMed).

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

  • 5,6-dihydro-5-azacytidine_Cancer Epigenetics Society (CES)
  • 5-fluoro-2′-deoxycytidine_Cancer Epigenetics Society (CES)
  • Genistein_Cancer Epigenetics Society (CES)

*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: AML: Acute Myeloid Leukemia; CLL: Chronic Lymphocytic Leukemia; CML: Chronic Myeloid Leukemia; CMML: Chronic myelomonocytic leukemia; MDS: Myelodysplastic Syndrome; MM: Multiple Myeloma; NSCLC: Non-Small Cell Lung Cancer; SLL: Small Lymphocytic Lymphoma. Roman numbers between brackets denote Phase I, II, or III clinical trials. Whenever available, clinical trial ID number and a link to the clinical trial’s details are provided.