Related Experiment Video
Updated: Jun 21, 2026

Using Multi-fluorinated Bile Acids and In Vivo Magnetic Resonance Imaging to Measure Bile Acid Transport
Published on: November 27, 2016
Identification of interspecies difference in hepatobiliary transporters to improve extrapolation of human biliary
1Pfizer Global Research & Development, Pfizer, Inc., Department of Pharmacokinetic, Dynamics, & Metabolism, St Louis Laboratory, 700 Chesterfield Parkway West, St Louis Chesterfield, MO 63017, USA. yurong.lai@pfizer.com
Abstract:
Increasing challenges include the application of in vitro/in vivo models for prediction of safety and pharmacokinetic profiles for the compounds entering drug development that are mainly secreted from bile. Species differences in biliary excretion have long been recognized and complicate the extrapolation of human pharmacokinetics from preclinical species or in vitro models. The currently available literature has been reviewed with a focus on drug-drug interactions mediated by hepatic drug transporters and the available tools for transporter assessments. Therefore, our incomplete understanding of interspecies differences and in vitro liver models poses a serious challenge in predicting human pharmacokinetics and/or safety profiles when the compounds are predominantly secreted from bile. This review outlines species differences in hepatobiliary secretion and the recent effort in understanding the absolute difference in hepatobiliary transporter expressions across species. In addition, understanding the expression of hepatobiliary transporters between in vitro hepatocyte models and in vivo to improve the prediction of biliary secretion is also discussed.
Related Concept Videos
Hepatic Drug Clearance: Role of Transporters
Physiological Pharmacokinetic Models: Incorporating Hepatic Transporter-Mediated Clearance
A recent model describes pravastatin's hepatobiliary excretion, mediated...
Hepatic Drug Excretion: Influencing Factors
Hepatic Drug Excretion: Enterohepatic Cycling
Post-release drugs and metabolites can be reabsorbed into the body from the intestine. For conjugated metabolites like glucuronides, reabsorption requires enzymatic hydrolysis by intestinal microflora. This...
Carrier-Mediated Transport
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters

