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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.

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