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Pharmaceuticals 2010, 3(7), 2022-2044; doi:10.3390/ph3072022

Demethylating Agents in the Treatment of Cancer

University of South Alabama, Mitchell Cancer Institute/1660 Springhill Ave., Mobile, AL 36604, USA
Author to whom correspondence should be addressed.
Received: 4 May 2010 / Revised: 22 June 2010 / Accepted: 29 June 2010 / Published: 2 July 2010
(This article belongs to the Special Issue Targeted Therapy)
View Full-Text   |   Download PDF [157 KB, uploaded 2 July 2010]


Gene silencing resulting from aberrant DNA methylation can lead to tumorigenesis. Therefore, drugs that inhibit or interfere with DNA methylation have been used to reactivate and induce silenced gene re-expression in malignancies. Two demethylating agents, azacitidine and decitabine, are approved for the treatment of myelodysplastic syndromes (MDS) by the U.S. Food and Drug Administration (FDA), and are now considered the standard of care in MDS. In this review, we discuss clinical data, including clinical benefits and toxicities, which led to the approval of azacitidine and decitabine. We also summarize findings from clinical trials that used these two demethylating agents in the treatment of solid tumors. Lastly, we discuss some limitations in the use of azacitidine and decitabine in cancer therapy.
Keywords: azacitidine; cancer; decitabine; epigenetics; methylation azacitidine; cancer; decitabine; epigenetics; methylation
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Howell, P.M., Jr.; Liu, Z.; Khong, H.T. Demethylating Agents in the Treatment of Cancer. Pharmaceuticals 2010, 3, 2022-2044.

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