Preclinical Profiling of Modified Oligonucleotides: Anticoagulation and Pharmacokinetic Properties

Backbone, sugar and pendant-group modifications were shown to influence the anticoagulant properties of a 20-mer oligonucleotide in human plasma in vitro. The pharmacokinetics, tissue-distribution and metabolism of a chimeric oligonucleotide (CGP 69845A), which had reduced anticoagulation properties...

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Veröffentlicht in:Nucleosides & nucleotides 1997-07, Vol.16 (7-9), p.1145-1153
Hauptverfasser: Nicklin, Paul L., Ambler, John, Mitchelson, Andrew, Bayley, Deborah, Phillips, Judy A., Craig, Sarah J., Mania, Brett P.
Format: Artikel
Sprache:eng
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Zusammenfassung:Backbone, sugar and pendant-group modifications were shown to influence the anticoagulant properties of a 20-mer oligonucleotide in human plasma in vitro. The pharmacokinetics, tissue-distribution and metabolism of a chimeric oligonucleotide (CGP 69845A), which had reduced anticoagulation properties, were compared with the analogous phosphorothioate oligodeoxynucleotide (CGP 69846A) in a tumour-bearing mouse model.
ISSN:0732-8311
DOI:10.1080/07328319708006150