Glucuronidation and sulfation are the most typical phase II metabolic reactions of drugs. The
resulting glucuronide and sulfate conjugates are generally considered inactive and safe …

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

Bioavailability of orally administered drugs is partly determined by function of drug
transporters in the liver and intestine. Therefore, we explored adenosine triphosphate …

Variability in individual capacity for hepatic elimination of therapeutic drugs is well
recognized and is associated with variable expression and activity of liver enzymes and …

Predicting transporter-based drug clearance (CL) and tissue concentrations (TC) in humans
is important to reduce the risk of failure during drug development. In addition, when …

The effect of membrane transporters on drug disposition, efficacy and safety is now well
recognized. Since the initial publication from the International Transporter Consortium …

This white paper examines recent progress, applications, and challenges in predicting
unbound and total tissue and intra/subcellular drug concentrations using in vitro and …

Bile salt export pump (BSEP) inhibition has emerged as an important mechanism that may
contribute to the initiation of human drug‐induced liver injury (DILI). Proactive evaluation …

Previous studies have shown that lipid-lowering statins are transported by various ATP-
binding cassette (ABC) transporters. However, because of varying methods, it is difficult to …

OATP1B1 (SLCO1B1) is predominantly expressed at the basolateral membrane of
hepatocytes and is critically important for the hepatic uptake and clearance of numerous …