Demethylating Agents in the Treatment of Cancer

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 fo...

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Published inPharmaceuticals Vol. 3; no. 7; pp. 2022 - 2044
Main Authors Howell, Paul M, Liu, Zixing, Khong, Hung T
Format Journal Article Book Review
LanguageEnglish
Published Switzerland MDPI AG 02.07.2010
MDPI
Subjects
azacitidine
cancer
decitabine
epigenetics
methylation
Review
cancer
decitabine
methylation
azacitidine
epigenetics
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Summary: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.
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ISSN:1424-8247
1424-8247
DOI:10.3390/ph3072022