In Vitro Drug Metabolism Using Liver Microsomes

Kathleen Knights, David Stresser, John Miners, Charles Crespi

    Research output: Chapter in Book/Report/Conference proceedingChapterpeer-review

    19 Citations (Scopus)

    Abstract

    Knowledge of the metabolic stability of newly discovered drug candidates eliminated by metabolism is essential for predicting the pharmacokinetic (PK) parameters that underpin dosing and dosage frequency. Further, characterization of the enzyme(s) responsible for metabolism (reaction phenotyping) allows prediction, at least at the qualitative level, of factors (including metabolic drug-drug interactions) likely to alter the clearance of both new chemical entities (NCEs) and established drugs. Microsomes are typically used as the enzyme source for the measurement of metabolic stability and for reaction phenotyping because they express the major drug-metabolizing enzymes cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT), along with others that contribute to drug metabolism. Described in this unit are methods for microsome isolation, as well as for the determination of metabolic stability and metabolite formation (including kinetics).

    Original languageEnglish
    Title of host publicationCurrent Protocols in Pharmacology
    PublisherJohn Wiley and Sons Inc.
    Pages7.8.1-7.8.24
    Number of pages24
    Volume2016
    ISBN (Print)9780471141754
    DOIs
    Publication statusPublished - 2016

    Publication series

    NameCurrent Protocols in Pharmacology
    ISSN (Print)1934-8282

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