In Vitro Techniques to Study Drug–Drug Interactions Involving Transport: Caco-2 Model for Study of P-Glycoprotein and Other Transporters

  • William R. Proctor
  • Xin Ming
  • Dhiren R. Thakker


Transporters play a pivotal role in defining disposition, therapeutic outcome, and adverse reactions of medicines. P-glycoprotein (P-gp) is an efflux transporter that is constitutively expressed in barrier tissues and excretory organs, and has wide substrate specificity; consequently, it may be responsible for wide-ranging drug–drug interactions (DDIs). This chapter critically evaluates the utility and limitations of Caco-2 cells, a model for human intestinal epithelium that expresses most intestinal transporters, in assessing DDIs mediated by P-gp and other transporters.


Permeability Glutathione Paclitaxel Doxorubicin Mannitol 
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Copyright information

© Springer Science+Business Media, LLC 2010

Authors and Affiliations

  • William R. Proctor
    • 1
  • Xin Ming
    • 1
  • Dhiren R. Thakker
    • 1
  1. 1.Division of Molecular Pharmaceutics, Eshelman School of PharmacyThe University of North Carolina at Chapel HillChapel HillUSA

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