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ITC recommendations for transporter kinetic parameter estimation and translational modeling of transport-mediated PK and DDIs in humans.


ABSTRACT: This white paper provides a critical analysis of methods for estimating transporter kinetics and recommendations on proper parameter calculation in various experimental systems. Rational interpretation of transporter-knockout animal findings and application of static and dynamic physiologically based modeling approaches for prediction of human transporter-mediated pharmacokinetics and drug-drug interactions (DDIs) are presented. The objective is to provide appropriate guidance for the use of in vitro, in vivo, and modeling tools in translational transporter science.

SUBMITTER: Zamek-Gliszczynski MJ 

PROVIDER: S-EPMC3898877 | biostudies-literature | 2013 Jul

REPOSITORIES: biostudies-literature

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ITC recommendations for transporter kinetic parameter estimation and translational modeling of transport-mediated PK and DDIs in humans.

Zamek-Gliszczynski M J MJ   Lee C A CA   Poirier A A   Bentz J J   Chu X X   Ellens H H   Ishikawa T T   Jamei M M   Kalvass J C JC   Nagar S S   Pang K S KS   Korzekwa K K   Swaan P W PW   Taub M E ME   Zhao P P   Galetin A A  

Clinical pharmacology and therapeutics 20130225 1


This white paper provides a critical analysis of methods for estimating transporter kinetics and recommendations on proper parameter calculation in various experimental systems. Rational interpretation of transporter-knockout animal findings and application of static and dynamic physiologically based modeling approaches for prediction of human transporter-mediated pharmacokinetics and drug-drug interactions (DDIs) are presented. The objective is to provide appropriate guidance for the use of in  ...[more]

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