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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
1999-12-13
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pubmed:abstractText |
Aptamers are oligonucleotide ligands selected, in vitro, to bind a specified target protein. The first aptamer to reach human clinical testing is NX1838, a polyethylene glycol conjugated aptamer that inhibits vascular endothelial growth factor. This paper describes the validation of a high-performance liquid chromatographic anion-exchange method for the determination of NX1838 in plasma. Measurements of intact NX1838 had a coefficient of variation of less than 8% and an accuracy between 107% and 115%. The assay was utilized to determine NX1838 plasma pharmacokinetics in rhesus monkeys following a single 1 mg/kg intravenous or subcutaneous dose. Following intravenous administration, the maximum achieved plasma concentration was 25.5 microg/ml with a terminal half-life of 9.3 h and clearance rate of 6.2 ml/h. After subcutaneous administration, the fraction of the dose absorbed into the plasma compartment was 0.78 with a time to peak concentration (4.9 microg/ml) of 8 to 12 h.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
1387-2273
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
10
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pubmed:volume |
732
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
203-12
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:10517237-Animals,
pubmed-meshheading:10517237-Chromatography, High Pressure Liquid,
pubmed-meshheading:10517237-Drug Stability,
pubmed-meshheading:10517237-Endothelial Growth Factors,
pubmed-meshheading:10517237-Humans,
pubmed-meshheading:10517237-Injections, Intravenous,
pubmed-meshheading:10517237-Injections, Subcutaneous,
pubmed-meshheading:10517237-Lymphokines,
pubmed-meshheading:10517237-Macaca mulatta,
pubmed-meshheading:10517237-Oligonucleotides,
pubmed-meshheading:10517237-Quality Control,
pubmed-meshheading:10517237-Reproducibility of Results,
pubmed-meshheading:10517237-Vascular Endothelial Growth Factor A,
pubmed-meshheading:10517237-Vascular Endothelial Growth Factors
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pubmed:year |
1999
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pubmed:articleTitle |
Detection and plasma pharmacokinetics of an anti-vascular endothelial growth factor oligonucleotide-aptamer (NX1838) in rhesus monkeys.
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pubmed:affiliation |
NeXstar Pharmaceuticals Inc., Boulder, CO 80301, USA.
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pubmed:publicationType |
Journal Article
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