Cytochrome P450 Mediated Drug Metabolism

Lars Olsen, Flemming Steen Jørgensen, Chris Oostenbrink

    Abstract

    Cytochrome P450 enzymes (CYPs) metabolize the majority of small molecule drug compounds. They catalyze a wide variety of chemical reactions, and potentially, a large number of different metabolites can be generated. Due to the promiscuous nature of the CYPs, it is not trivial to predict what metabolites are generated. It is, however, important to know where a compound is metabolized and which metabolites are formed. This gives the possibility to redesign the compound if it is too rapidly metabolized or to avoid the formation of toxic metabolites. These questions are important both for understanding the action of known drugs (including drug-drug interactions, an important issue in adverse drug reactions) and for the development of new and/or improved drugs. In this chapter we will discuss in silico methods for prediction of the sites of metabolism with an emphasis on how the compounds bind and how easily a site in the compounds reacts with the enzyme.

    Original languageEnglish
    Title of host publicationNew Horizons in Predictive Drug Metabolism and Pharmacokinetics
    EditorsAlan G.E. Wilson
    Number of pages13
    Place of PublicationCambridge
    PublisherRoyal Society of Chemistry
    Publication date2016
    Pages66-78
    Chapter4
    ISBN (Print)978-1-84973-828-6
    ISBN (Electronic)978-1-78262-237-6
    Publication statusPublished - 2016
    SeriesRSC Drug Discovery
    Volume49

    Keywords

    • Former Faculty of Pharmaceutical Sciences
    • Faculty of Health and Medical Sciences

    Fingerprint

    Dive into the research topics of 'Cytochrome P450 Mediated Drug Metabolism'. Together they form a unique fingerprint.

    Cite this