With efforts to reduce cytochrome P450-mediated clearance (CL) during the early stages of
drug discovery, transporter-mediated CL mechanisms are becoming more prevalent …

Interindividual variability in activity of uptake transporters is evident in vivo, yet limited data
exist in vitro, confounding in vitro-in vivo extrapolation. The uptake kinetics of seven organic …

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

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 …

Abstract Background and Objectives The interplay between liver metabolising enzymes and
transporters is a complex process involving system-related parameters such as liver blood …

In contrast to primary hepatocytes, estimating carrier-mediated hepatic disposition by using
a panel of single transfected cell-lines provides direct information on the contribution of the …

To assess the feasibility of using sandwich-cultured human hepatocytes (SCHHs) as a
model to characterize transport kinetics for in vivo pharmacokinetic prediction, the …

This review illustrates the concept of a rate-determining process in the overall hepatic
elimination of anionic drugs that involves transporters in the uptake process. A kinetic study …

Purpose To develop physiologically based pharmacokinetic (PBPK) model to predict the
pharmacokinetics and drug-drug interactions (DDI) of pravastatin, using the in vitro transport …

The ability to predict hepatic metabolic clearance is a key component in the design and
selection of small molecule drug candidates within the pharmaceutical industry. The …