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Induction of cytochrome P450 enzymes, especially CYP3A4, could be a significant clinical issue leading to therapeutic efficacy reduction or even loss of a co-medication or the CYP3A4 inducer itself, because CYP3A4 alone is involved in the metabolism of more than 50% of marketed drugs. In this chapter, the mechanism of action of CYP induction, clinical consequence, screening strategies and the structures of representative CYP inducers are briefly described. The chapter focuses on the mitigation strategies for CYP3A4 and CYP1A2 inductions with many literature examples illustrated: (1) introducing a polar substituent to the hydrophobic group; (2) removing or replacing the key hydrophobic group with a less hydrophobic group; and (3) introducing steric hindrance or rigidifying the structure.

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