Ageing is characterized by a progressive decline in the functional reserve of multiple organs
and systems, which can influence drug disposition. In addition, comorbidity and …

Introduction: The sandwich-cultured hepatocyte (SCH) model has become an invaluable in
vitro tool for studying hepatic drug transport, metabolism, biliary excretion and toxicity. The …

The utilization of in vitro data to predict drug pharmacokinetics (PK) in vivo has been a
consistent practice in early drug discovery for decades. However, its success is hampered …

Breast cancer resistance protein (BCRP), an efflux transporter expressed at the bile
canalicular membrane, is responsible for the biliary clearance of many drugs. Data on the …

The well‐stirred hepatic clearance model (WSHM) has been expanded to include drug
transporters (ie, extended clearance model [ECM]). However, the consequences of this …

Early prediction of human pharmacokinetics (PK) and drug–drug interactions (DDI) in drug
discovery and development allows for more informed decision making. Physiologically …

Using positron emission tomography imaging, we determined the hepatic concentrations
and hepatobiliary transport of [11C] rosuvastatin (RSV; iv injection) in the absence (n= 6) …

Multidrug-associated protein 2 (MRP2) is an efflux transporter that is expressed at the bile
canalicular membrane. To allow in vitro to in vivo extrapolation of the contribution of MRP2 …

In recent years, the functional interplay between drug-metabolizing enzymes (DMEs) and
drug transporters (DTs) in drug absorption and disposition, as well as the complex drug …

Hepatic clearance (CL H) prediction is a critical parameter to estimate human dose.
However, CL H underpredictions are common, especially for slowly metabolized drugs, and …