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 …

Hepatobiliary transport mechanisms have been identified to play a significant role in
determining the systemic clearance for a number of widely prescribed drugs and an …

Determining the biliary clearance of drugs in humans is very challenging because bile is not
readily accessible due to the anatomy of the hepatobiliary tract. The collection of bile usually …

Objectives Membrane transporters and metabolism are major determinants of the
hepatobiliary elimination of drugs. This work investigates several key questions for drug …

Well-established techniques are available to predict in vivo hepatic uptake and metabolism
from in vitro data, but predictive models for biliary clearance remain elusive. Several studies …

Previously we have reported that hepatobiliary transporter expressions in sandwich cultured
hepatocytes (SCH) are altered 2-to 5-fold. This change could limit the model's predictive …

Hepatobiliary elimination can be a major clearance pathway dictating the pharmacokinetics
of drugs. Here, we first compared the dose eliminated in bile in preclinical species (monkey …

Transporter-mediated alterations in bile acid disposition may have significant toxicological
implications. Current methods to predict interactions are limited by the interplay of multiple …

Introduction: Impaired bile formation leads to the accumulation of cytotoxic bile salts in
hepatocytes and, consequently, cholestasis and severe liver disease. Knowledge of the role …

Abstract Evaluation of hepatobiliary transport of drugs is an important challenge, notably
during the development of new molecular identities. In this context, sandwich-cultured …