Cytochrome P-450-Dependent Oxidative Cleavage of 1-(Tetrahydro-2-Furanyl)-5-Fluorouracil to 5-Fluorouracil
نویسندگان
چکیده
منابع مشابه
Metabolic activation of R,S-1-(tetrahydro-2-furanyl)-5-fluorouracil (ftorafur) to 5-fluorouracil by soluble enzymes.
There are two major R,S-1-(tetrahydro-2-furanyl)-5-fluorouracil (ftorafur) activation pathways to 5-fluorouracil, one that is mediated by microsomal cytochrome P-450 oxidation at C-5' of the tetrahydrofuran moiety and one that is mediated by soluble enzymes. This report demonstrates that the soluble enzyme pathway proceeds via enzymatic cleavage (possibly hydrolytic) of the N-1--C-2' bond to yi...
متن کامل5-Fluorouracil concentrations in human plasma following R,S-1-(tetrahydro-2-furanyl)-5-fluorouracil (ftorafur) administration.
Following administration of i.v. doses of fl,S-1 -(tetrahydro-2furanyl)-5-fluorouracil in cancer patients, discrepant results have been obtained by several investigators when assaying for 5-fluorouracil (FUra) plasma concentrations, ranging from 0.1 to 5 fig/ml at peak concentrations. The newly isolated fl,S-1(tetrahydro-2-furanyl)-5-fluorouracil metabolites with altered tetrahydrofuran moiety ...
متن کاملDisposition and Metabolism of 1-(Tetrahydro-2-furanyl)-5-fluorouracil (Ftorafur) in Humans1
The pharmacology of high-dose 1-(tetrahydro-2-furanyl)5-fluorouracil (FT) has been studied by radiochemical and Chromatographie techniques in eight patients. Plasma disappearance of FT was exponential, with a half-life of 8.8 hr. Plasma concentrations of 5-fluorouracil (FUra) were sustained at 12.8 nmol/ml (1.7 /¿g/ml) for at least 48 hr after FT administration. The concentrations of FUra deri...
متن کاملDisposition and metabolism of 1-(tetrahydro-2-furanyl)-5-fluorouracil (ftorafur) in humans.
The pharmacology of high-dose 1-(tetrahydro-2-furanyl)-5-fluorouracil (FT) has been studied by radiochemical and chromatographic techniques in eight patients. Plasma disappearance of FT was exponential, with a half-life of 8.8 hr. Plasma concentrations of 5-fluorouracil (FUra) were sustained at 12.8 nmol/ml (1.7 microgram/ml) for at least 48 hr after FT administration. The concentrations of FUr...
متن کاملBioactivation of tegafur to 5-fluorouracil is catalyzed by cytochrome P-450 2A6 in human liver microsomes in vitro.
Tegafur is a prodrug of 5-fluorouracil (5-FU) consisting of a new class of oral chemotherapeutic agents, tegafur/uracil and S-1, which are classified as dihydropyrimidine dehydrogenase inhibitory fluoropyrimidines. It is bioactivated to 5-FU via 5'-hydroxylation mediated by cytochrome P-450 (CYP). However, which isoform(s) of CYP is responsible for the bioactivation process of tegafur remains u...
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ژورنال
عنوان ژورنال: Japanese Journal of Pharmacology
سال: 1984
ISSN: 0021-5198
DOI: 10.1254/jjp.36.43