Drug metabolism often represents a major source of inter-individual variability in drug response.  A root case for differences in drug metabolism is due to an alteration of cytochrome P450 (CYP) enzymatic activity. Cytochrome P450 enzymes, in particular CYP3A4, are responsible for the bulk of the metabolism of known drugs in humans. As a consequence, changes in the catalytic activity of these enzymes by co-administered drugs can lead to variability in drug exposure. Today the evaluation of the potential of a drug candidate to alter CYP enzyme activity represents an important part of pharmaceutical drug Development process. The goal of these studies are to predict the magnitude of clinical drug-drug interactions (DDI) involving the modulation of the activities of these enzymes. The current presentation will examine ADME activities beyond the common strategies and decision making processes for the assessment of DDI risk in pharmaceutical development.

Metabolic clearance by CYP450 metabolism

243rd National Meeting (2012)

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