SGI-110. DNA methyltransferase inhibitor, oncolytic

E. A. Griffiths, G. Choy, S. Redkar, P. Taverna, M. Azab, Adam R Karpf

Research output: Contribution to journalArticle

27 Citations (Scopus)

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 genespecific 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.

Original languageEnglish (US)
Pages (from-to)535-543
Number of pages9
JournalDrugs of the Future
Volume38
Issue number8
DOIs
StatePublished - Aug 2013

Fingerprint

decitabine
Methyltransferases
DNA
Pharmaceutical Preparations
Phase II Clinical Trials
Clinical Trials, Phase I
Deamination
Deoxyguanosine
Myelodysplastic Syndromes
Prodrugs
Platinum
Nucleosides
Acute Myeloid Leukemia
Oligonucleotides
Ovarian Neoplasms
Hepatocellular Carcinoma
Animal Models
SGI-110

Keywords

  • Acute myeloid leukemia
  • Hepatocellular carcinoma
  • Hypomethylating prodrug
  • Myelodysplastic syndrome
  • Ovarian cancer
  • SGI-110

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

Cite this

Griffiths, E. A., Choy, G., Redkar, S., Taverna, P., Azab, M., & Karpf, A. R. (2013). SGI-110. DNA methyltransferase inhibitor, oncolytic. Drugs of the Future, 38(8), 535-543. https://doi.org/10.1358/dof.2013.038.08.1980499

SGI-110. DNA methyltransferase inhibitor, oncolytic. / Griffiths, E. A.; Choy, G.; Redkar, S.; Taverna, P.; Azab, M.; Karpf, Adam R.

In: Drugs of the Future, Vol. 38, No. 8, 08.2013, p. 535-543.

Research output: Contribution to journalArticle

Griffiths, EA, Choy, G, Redkar, S, Taverna, P, Azab, M & Karpf, AR 2013, 'SGI-110. DNA methyltransferase inhibitor, oncolytic', Drugs of the Future, vol. 38, no. 8, pp. 535-543. https://doi.org/10.1358/dof.2013.038.08.1980499
Griffiths, E. A. ; Choy, G. ; Redkar, S. ; Taverna, P. ; Azab, M. ; Karpf, Adam R. / SGI-110. DNA methyltransferase inhibitor, oncolytic. In: Drugs of the Future. 2013 ; Vol. 38, No. 8. pp. 535-543.
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