Solute carrier (SLC) transporters present as the loci of important drug–drug interactions
(DDIs). Therefore, sponsors generate in vitro half‐maximal inhibitory concentration (IC50) …

The derivation of safe levels of exposure in humans for compounds that are assumed to
cause threshold toxicity has relied on the application of a 100-fold uncertainty factor to a …

Introduction Transporters are significant in dictating drug pharmacokinetics, thus inhibition of
transporter function can alter drug concentrations resulting in drug-drug interactions (DDIs) …

Drug transporters are recognized widely for their role in clinical pharmacokinetics and drug–
drug interactions (DDIs). This has provided impetus to the inclusion of transporter substrate …

Improving drug translation is becoming a top priority as research and development costs
keep increasing. It typically takes 10–20 years and a couple of billion dollars to bring a new …

Intestinal first-pass metabolism may contribute to low oral drug bioavailability and drug-drug
interactions, particularly for CYP3A substrates. The current analysis predicted intestinal …

Over the last 5 years the quantification of transporter-protein absolute abundances has
dramatically increased in parallel to the expanded use of in vitro–in vivo extrapolation …

Caco-2 screens are routinely used in laboratories to measure the permeability of
compounds and can identify substrates of efflux transporters. In this study, we hypothesized …

This white paper provides updated International Transporter Consortium (ITC)
recommendations on transporters that are important in drug development following the 3rd …

Concepts in risk assessment practice are expressed in terms of external exposure, while
internal exposure determines whether toxic effects will occur. Often only a fraction of the …