Tactics to avoid inhibition of cytochrome P450s

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


This chapter will focus on avoiding inhibition of cytochrome P450s. This problem leads to drug–drug interactions that can severely restrict the patients who can receive a particular drug. The first sections [(1) background and motivation, (2) the structure of the cytochrome P450s, and (3) overview of the mechanism of cytochrome P450s] provide essential background to understanding both the problem and some of the solutions. The subsequent three sections [(4) trends for inhibition to be modulated by bulk properties (database analysis), (5) metal chelation, and (6) reactive metabolites and mechanism-based inhibition] will outline some general methods for tackling the problem, and each section has a summary in which the strategic approaches that follow from the information are presented. In the final section [(7) examples of successful reduction of P450 liability], how these strategies can be reduced to tactical application is illustrated with published examples.
Original languageEnglish
Title of host publicationTactics in contemporary drug design
EditorsNicholas A. Meanwell
Place of PublicationHeidelberg, New York, Dordrecht, London
PublisherSpringer Nature
Number of pages52
ISBN (Electronic)9783642550416
ISBN (Print)9783642550409
Publication statusPublished - 2015

Publication series

NameTopics in Medicinal Chemistry Series


  • Cytochrome P450
  • Inhibition
  • Lead optimization
  • Medicinal chemistry


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