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- W1569591709 abstract "One important aspect of drug safety is the extent to which a new drug entity (NDE) causes metabolism-based pharmacokinetic interactions with co-administered medications. Therefore, potential drug-drug interactions may be tested for each enzyme of interest with a suitable probe substrate. The validity of these assays depends on the use of human enzymes and the probe substrate/assay conditions measuring the activity of the subject enzyme with a high degree of specificity. However, if enzyme mixtures, such as human fiver microsomes, are to be used probe substrate choices are more limited, as substrates with multiple pathways of metabolism are usually inappropriate. The chapter discusses some general considerations for conducting fluorometric cytochrome P450 enzyme (CYP) inhibition assays and then provides a general method for conducting the assay for several of the drug-metabolizing CYPs. Assays should be conducted under initial rate conditions formation of the metabolite should be linear with respect to enzyme concentration and incubation time, and the total consumption of the substrate should be less than 20%." @default.
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- W1569591709 date "2002-01-01" @default.
- W1569591709 modified "2023-10-11" @default.
- W1569591709 title "Design and application of fluorometric assays for human cytochrome P450 inhibition" @default.
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- W1569591709 doi "https://doi.org/10.1016/s0076-6879(02)57685-0" @default.
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