Membrane transporters play diverse roles in the pharmacokinetics and pharmacodynamics
of small‐molecule drugs. Understanding the mechanisms of drug‐transporter interactions at …

Increasing challenges include the application of in vitro/in vivo models for prediction of
safety and pharmacokinetic profiles for the compounds entering drug development that are …

Unmanageable severe adverse events caused by drug‐drug interactions (DDIs), leading to
market withdrawals or restrictions in the clinical usage, are increasingly avoided with the …

Membrane transporters play an important role in the absorption, distribution, metabolism,
and excretion of xenobiotic substrates, as well as endogenous compounds. The evaluation …

Active transport across biological membranes represents a critical step in the disposition of
many drugs. It is now well-established that different efflux and uptake transporters such as P …

This white paper provides a critical analysis of methods for estimating transporter kinetics
and recommendations on proper parameter calculation in various experimental systems …

Drug transporters expressed in liver and kidney play a critical role in the elimination of a
wide range of drugs and xenobiotics and inhibition of these transporters may therefore …

Hepatic efflux transporters include numerous well-known and emerging proteins localized to
the canalicular or basolateral membrane of the hepatocyte that are responsible for the …

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 …

Together with drug metabolising enzymes, transmembrane transporters are important
determinants of drug metabolism and drug clearance by the liver. Hepatic uptake of organic …