Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
6C
pubmed:dateCreated
2005-12-7
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.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0250-7005
pubmed:author
pubmed:issnType
Print
pubmed:volume
25
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
4487-92
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:articleTitle
Excretion of hydroxylated metabolites of tamoxifen in human bile and urine.
pubmed:affiliation
Section for Endocrinology, Institute of Medicine, University of Bergen, Bergen, Norway.
pubmed:publicationType
Journal Article, Case Reports, Research Support, Non-U.S. Gov't