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CYP2C9 Ile359 and Leu359 variants: enzyme kinetic study with seven substrates.
TLDR
The results indicate that the Ile359 to Leu359 change significantly decreases the catalytic activity of all the CYP2C9-mediated metabolisms studied, whereas the extent of the reduction in activity and changes of the kinetic parameters varies between substrates.
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Oxidative metabolism of omeprazole in human liver microsomes: cosegregation with S-mephenytoin 4'-hydroxylation.
TLDR
It is suggested that S-mephenytoin 4'-hydroxylase is an enzyme primarily responsible for the 5-Hydroxylation of OPz and further metabolism of OPZ-SFN, but not for the sulfoxidation ofOPZ in human liver microsomes.
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Effects of CYP2C19 genotypic differences in the metabolism of omeprazole and rabeprazole on intragastric pH
Omeprazole is mainly metabolized in the liver by CYP2C19, a genetically determined enzyme, whereas rabeprazole is mainly reduced non‐enzymatically and partially metabolized by CYP2C19. The…
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Human buprenorphine N-dealkylation is catalyzed by cytochrome P450 3A4.
TLDR
The demonstration of BN N-dealkylation by recombinant CYP3A4 and the agreement in the affinities (apparent KM values) of human liver microsomes and recombinant cytochrome P450 enzyme(s) provide the most supportive evidence for BNN-dealksylation being catalyzed by CYP 3A4.
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Sertraline N-demethylation is catalyzed by multiple isoforms of human cytochrome P-450 in vitro.
TLDR
Sertraline N-demethylation activities were detected in all cDNA-expressed CYP isoforms studied and that the contribution of any individual isoform does not exceed 40% of overall metabolism is suggested.
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The effects of selective serotonin reuptake inhibitors and their metabolites on S-mephenytoin 4'-hydroxylase activity in human liver microsomes.
TLDR
It is suggested that some SSRIs and their metabolites with a low Ki value may reduce the clearance of drugs metabolized by this isoform of P450, thereby resulting in a possible drug-drug interaction, when administered simultaneously.
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Disposition kinetics and metabolism of omeprazole in extensive and poor metabolizers of S-mephenytoin 4'-hydroxylation recruited from an Oriental population.
TLDR
The kinetic variables of omeprazole and its two primary metabolites in plasma and the excretion profile of its principal metabolite in urine were examined and the log10 4'-hydroxymephenytoin excreted in urine correlated significantly (P less than .01) with the apparent p.o. Clearance in PMs.
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Effects of clarithromycin on the metabolism of omeprazole in relation to CYP2C19 genotype status in humans
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pH‐dependent uptake of irinotecan and its active metabolite, SN‐38, by intestinal cells
TLDR
CPT‐11 and SN‐38 have absorption characteristics of weakly basic drugs such as short‐chain fatty acids, suggesting that alkalization of the intestinal lumen may be critical to reduce their reabsorption and associated side effects.
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Bioactivation of tegafur to 5-fluorouracil is catalyzed by cytochrome P-450 2A6 in human liver microsomes in vitro.
TLDR
Findings clearly suggest that CYP2A6 is a principal enzyme responsible for the bioactivation process of tegafur in human liver microsomes and cDNA-expressed human CYPs.
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