Pl. Nicklin et al., PRECLINICAL PROFILING OF MODIFIED OLIGONUCLEOTIDES - ANTICOAGULATION AND PHARMACOKINETIC PROPERTIES, Nucleosides & nucleotides, 16(7-9), 1997, pp. 1145-1153
Backbone, sugar and pendant-group modifications were shown to influenc
e the anticoagulant properties of a 20-mer oligonucleotide in human pl
asma in vitro. The pharmacokinetics, tissue-distribution and metabolis
m of a chimeric oligonucleotide (CGP 69845A), which had reduced antico
agulation properties, were compared with the analogous phosphorothioat
e oligodeoxynucleotide (CGP 69846A) in a tumour-bearing mouse model.