Source:http://linkedlifedata.com/resource/pubmed/id/16334131
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6C
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pubmed:dateCreated |
2005-12-7
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pubmed:abstractText |
The selective oestrogen-receptor modulator tamoxifen is the most commonly used drug against breast cancer. It has potent metabolites, such as 4-hydroxytamoxifen. Recently, the metabolite 4-hydroxy-N-desmethyltamoxifen has received increased attention as it may be a major contributor to the overall effects of tamoxifen. The excretion of tamoxifen and its metabolites was examined in a patient with biliary drainage after an oral dose of [14C]tamoxifen. During the first 10 days after oral dosing, 11.5, 26.7 and 24.7% of the radioactivity was excreted in the bile, urine and faeces, respectively. After deconjugation with beta-glucuronidase, the concentrations of tamoxifen and 4 of its metabolites were measured, and it was observed that the hydroxylated metabolites were excreted in the bile and urine. 4-Hydroxytamoxifen was the dominant compound, being detected during the first day of observation, whereas 4-hydroxy-N-desmethyltamoxifen was first observed in the urine and bile after 4 days. This is the first report on tamoxifen excretion in human bile and urine demonstrating that 4-hydroxytamoxifen may be a first-pass metabolite. In contrast, the potent metabolite 4-hydroxy-N-desmethyltamoxifen was first detected 4 days after administration of a single oral dose.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:issn |
0250-7005
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
25
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4487-92
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:16334131-Antineoplastic Agents, Hormonal,
pubmed-meshheading:16334131-Bile,
pubmed-meshheading:16334131-Feces,
pubmed-meshheading:16334131-Female,
pubmed-meshheading:16334131-Humans,
pubmed-meshheading:16334131-Middle Aged,
pubmed-meshheading:16334131-Pancreatic Neoplasms,
pubmed-meshheading:16334131-Tamoxifen
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pubmed:articleTitle |
Excretion of hydroxylated metabolites of tamoxifen in human bile and urine.
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pubmed:affiliation |
Section for Endocrinology, Institute of Medicine, University of Bergen, Bergen, Norway.
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pubmed:publicationType |
Journal Article,
Case Reports,
Research Support, Non-U.S. Gov't
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