Abstract Evaluation of drug–drug interaction (DDI) risk is vital to establish benefit–risk
profiles of investigational new drugs during drug development. In vitro experiments are …

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

Drug–drug interactions are a serious clinical issue. An important mechanism underlying
drug–drug interactions is induction or inhibition of drug transporters that mediate the cellular …

Several recent studies show that inhibition of the hepatic transport proteins organic anion-
transporting polypeptide 1B1 (OATP1B1) and 1B3 (OATP1B3) can result in clinically …

Quantitative prediction of complex drug-drug interactions (DDIs) involving hepatic
transporters and cytochromes P450 (P450s) is challenging. We evaluated the extent of DDIs …

Transporters govern the access of molecules to cells or their exit from cells, thereby
controlling the overall distribution of drugs to their intracellular site of action. Clinically …

The transporter-mediated uptake of drugs from blood into hepatocytes is a prerequisite for
intrahepatic drug action or intracellular drug metabolism before excretion. Therefore, uptake …

The absorption, distribution, metabolism, and excretion (ADME) of drugs in vivo are to a
large extent dependent on different transport and metabolism routes. Elucidation of this …

The risk assessment of organic anion transporting polypeptide (OATP) 1B1–mediated drug-
drug interactions (DDIs) is an indispensable part of drug development. We previously …

Current challenges with the in vitro–in vivo extrapolation (IVIVE) of hepatic uptake clearance
involving organic anion–transporting polypeptide (OATP) 1B1/1B3 hinder drug design …