Background: Intestinal drug metabolism and transport are now well recognized determinants of drug disposition in humans. During the last decade, various animal models lacking drug transporters have been generated in order to investigate the role of transporters for drug absorption, distribution and elimination.
Objective: In this review the use of the animal models for the investigation of intestinal drug transport will be discussed.
Methods: Publications describing the use of knockout animals (e.g., P-glycoprotein, Bcrp, and Oct1) regarding intestinal drug transport and animals characterized by mutations in transporters genes (e.g., Mrp2) were mainly considered for this review.
Results/conclusion: Knockout mouse models for ABC transporters are highly valuable tools to investigate the role of intestinal efflux transporters for the bioavailability of various compounds.