Absorptive transporter effects predominate

Absorptive and efflux transporter effects could be important

Figure 12 The biopharmaceutics classification system (BCS), as defined by Amidon et a/.157 and extended by Wu and Benet,158 showing the predominant routes of drug elimination and the transporter effects on drug disposition.

There was very little interest in the importance of drug transporters in drug bioavailability when the BCS was first developed. But the involvement of drug transport at all steps of the pharmacokinetic processes has provided a clearer correlation between the solubility and permeability of a drug and its fate within the human body. Hence the action of transporters is now included in ADMET predictive models.

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