CHAPTER 11: Strategies to Mitigate CYP450 Inhibition
Published:20 Aug 2021
A. G. Dossetter, M. J. de Groot, and S. E. Skerratt, in The Medicinal Chemist's Guide to Solving ADMET Challenges, ed. P. Schnider, The Royal Society of Chemistry, 2021, pp. 220-247.
Download citation file:
The cytochrome P450s (CYPs) comprise a superfamily of haem-containing proteins that are predominantly expressed in the liver and catalyse the metabolism of a broad range of exogenous and endogenous molecules. The inhibition of P450-mediated drug metabolism may result in undesirable elevations in plasma drug concentrations; therefore, an understanding of the potential for CYP inhibition is important from a therapeutic efficacy and safety stand-point. This chapter will highlight and exemplify medicinal chemistry strategies to reduce CYP inhibitory activity and hence the potential for drug–drug interactions.