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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
6
|
| pubmed:dateCreated |
1990-12-4
|
| pubmed:abstractText |
The experimental antineoplastic agent temozolomide was not metabolised in vitro at a measurable rate by mouse liver fractions. In contrast, the temozolomide analogue 3-methylbenzotriazinone was metabolically N-demethylated by hepatic microsomes to yield benzotriazinone. The major route of excretion of [14C]-labelled temozolomide in mice was via the kidneys. An acidic metabolite of temozolomide, probably a conjugate, was found in the urine of mice, but its identity could not be established unambiguously. Spectroscopic analysis and chemical tests revealed that it possesses an intact NNN-linkage. Another metabolite was found in the urine of patients but not of mice. This metabolite was identified as the 8-carboxylic acid derivative of temozolomide. Unlike the unknown species, this metabolite was cytotoxic against TLX5 lymphoma cells in vitro.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:issn |
0344-5704
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
26
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
429-36
|
| pubmed:dateRevised |
2006-11-15
|
| pubmed:meshHeading |
pubmed-meshheading:2225314-Animals,
pubmed-meshheading:2225314-Antineoplastic Agents,
pubmed-meshheading:2225314-Chromatography, High Pressure Liquid,
pubmed-meshheading:2225314-Dacarbazine,
pubmed-meshheading:2225314-Drug Evaluation,
pubmed-meshheading:2225314-Drug Screening Assays, Antitumor,
pubmed-meshheading:2225314-Humans,
pubmed-meshheading:2225314-Lymphoma,
pubmed-meshheading:2225314-Magnetic Resonance Spectroscopy,
pubmed-meshheading:2225314-Male,
pubmed-meshheading:2225314-Mass Spectrometry,
pubmed-meshheading:2225314-Mice,
pubmed-meshheading:2225314-Mice, Inbred BALB C,
pubmed-meshheading:2225314-Mice, Inbred CBA,
pubmed-meshheading:2225314-Microsomes, Liver,
pubmed-meshheading:2225314-Oxidation-Reduction,
pubmed-meshheading:2225314-Thymus Neoplasms,
pubmed-meshheading:2225314-Triazines,
pubmed-meshheading:2225314-Tumor Cells, Cultured
|
| pubmed:year |
1990
|
| pubmed:articleTitle |
Characterisation of urinary metabolites of temozolomide in humans and mice and evaluation of their cytotoxicity.
|
| pubmed:affiliation |
Cancer Research Campaign Experimental Chemotherapy Group, Pharmaceutical Sciences Institute, Aston University, Birmingham, England, U.K.
|
| pubmed:publicationType |
Journal Article,
Clinical Trial,
Comparative Study,
In Vitro,
Research Support, Non-U.S. Gov't
|