Physiologically‐based pharmacokinetic (PBPK) modeling has been extensively used to
quantitatively translate in vitro data and evaluate temporal effects from drug–drug interactions (…

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

Purpose Drug elimination in the liver consists of uptake, metabolism, biliary excretion, and
sinusoidal efflux from the hepatocytes to the blood. We aimed to establish an accurate …

… The activities of OCT1, OCT2, and OCT3 in these cells were confirmed in the previous
report (Umehara et al., 2007) and in this study again (data not shown). YM155 inhibited human …

Ritonavir is one of several ketoconazole alternatives used to evaluate strong CYP3A4 inhibition
potential in clinical drug–drug interaction (DDI) studies. In this study, four physiologically …

Background: The fraction of an absorbed drug metabolized by the different hepatic
cytochrome P450 (CYP) enzymes, relative to total hepatic CYP metabolism (fm CYP ), can be …

Esterases may play a major role in the clearance of drugs with functional groups amenable
to hydrolysis, particularly in the case of ester prodrugs. To understand the processes …

Total human clearance is a key determinant for the pharmacokinetic behavior of drug candidates.
Our group recently introduced the Extended Clearance Model (ECM) as an accurate in …

The generation of reliable kinetic parameters to describe P-glycoprotein (P-gp) activity is
essential for predicting the impact of efflux transport on gastrointestinal drug absorption. The …

This drug-drug interaction study determined the effect of cyclosporine, an inhibitor of organic
anion transporting polypeptide (OATP) 1B3 and P-gp, on the pharmacokinetics (PK) of …