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SGI-110: DNA Methyltransferase Inhibitor Oncolytic.


ABSTRACT: SGI-110 is a second-generation hypomethylating prodrug whose active metabolite is the well-characterized drug decitabine. This novel compound is an oligonucleotide consisting of decitabine linked through a phosphodiester bond to the endogenous nucleoside deoxyguanosine. The dinucleotide configuration provides protection from drug clearance by deamination, while maintaining at least equivalent effects on gene-specific and global hypomethylation both in vitro and in animal model systems. This agent is currently being tested in phase I and II clinical trials in humans and has been demonstrated to be safe and well tolerated as a single agent, with evidence of promising activity in heavily pretreated (including currently FDA approved hypomethylating drugs) myelodysplastic syndrome and acute myeloid leukemia patients. Ongoing trials are also open in platinum-resistant ovarian cancer and hepatocellular carcinoma.

SUBMITTER: Griffiths EA 

PROVIDER: S-EPMC4503259 | biostudies-literature | 2013 Aug

REPOSITORIES: biostudies-literature

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SGI-110: DNA Methyltransferase Inhibitor Oncolytic.

Griffiths E A EA   Choy G G   Redkar S S   Taverna P P   Azab M M   Karpf A R AR  

Drugs of the future 20130801 8


SGI-110 is a second-generation hypomethylating prodrug whose active metabolite is the well-characterized drug decitabine. This novel compound is an oligonucleotide consisting of decitabine linked through a phosphodiester bond to the endogenous nucleoside deoxyguanosine. The dinucleotide configuration provides protection from drug clearance by deamination, while maintaining at least equivalent effects on gene-specific and global hypomethylation both in vitro and in animal model systems. This agen  ...[more]

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