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SGI-110: DNA Methyltransferase Inhibitor Oncolytic
E A Griffiths1, G Choy2, S Redkar2
1Roswell Park Cancer Institute, Elm & Carlton Sts., Buffalo, New York 14263, USA.
Drugs of the Future
|July 21, 2015
Summary
SGI-110, a novel hypomethylating prodrug, shows promising safety and efficacy in clinical trials for myelodysplastic syndrome and acute myeloid leukemia. Its unique dinucleotide structure enhances stability and maintains therapeutic effects.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Decitabine is a well-characterized hypomethylating drug.
- Hypomethylating agents are crucial in treating hematological malignancies.
- Existing treatments face challenges with drug clearance and efficacy.
Purpose of the Study:
- To evaluate SGI-110, a novel hypomethylating prodrug, as a potential cancer therapeutic.
- To assess the safety, tolerability, and efficacy of SGI-110 in preclinical and clinical settings.
- To investigate the pharmacokinetic advantages of SGI-110's unique dinucleotide structure.
Main Methods:
- SGI-110, an oligonucleotide prodrug, was synthesized by linking decitabine to deoxyguanosine.
- In vitro and animal model systems were used to assess hypomethylation effects.
- Phase I and II clinical trials were conducted in human patients with various cancers.
Main Results:
- SGI-110 demonstrated protection from deamination-mediated clearance compared to decitabine.
- Equivalent or enhanced gene-specific and global hypomethylation effects were observed.
- The agent proved safe and well-tolerated as a single agent in clinical trials.
- Promising activity was noted in myelodysplastic syndrome and acute myeloid leukemia patients, including those pretreated with other hypomethylating drugs.
Conclusions:
- SGI-110 represents a promising second-generation hypomethylating agent with improved stability.
- Its safety and efficacy profile supports its continued investigation in hematological malignancies and other cancers.
- SGI-110 offers a potential new therapeutic option for patients with limited treatment alternatives.
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