Principal Scientist Genentech, Inc. South San Francisco, California
In vivo preclinical studies can provide insight into the involvement and specific roles of transporters in drug absorption and disposition and can be valuable complements to in vitro studies. Among in vivo transporter models, knock-out animals have provided essential understanding of the contributions of transporters to the disposition of drugs and endogenous substrates. Humanized transporter animal models have been available for about 10 years and have been expected to address limitations resulting from species differences in transporter expression and substrate specificity and allow more relevant and quantitative predictions of the impact of transporters on human pharmacokinetics. This presentation will review the humanized transporter models that have been developed and will provide examples of their potential applications and limitations.
- Have a general understanding of the humanized transporter models that have been developed.
- Describe the results obtained in the characterizations of humanized transporter models.
- Define the potential applications and limitations of humanized transporter models.