What do drug transporters really do?

SK Nigam - Nature reviews Drug discovery, 2015 - nature.com
Potential drug–drug interactions mediated by the ATP-binding cassette (ABC) transporter
and solute carrier (SLC) transporter families are of clinical and regulatory concern. However …

Clinical probes and endogenous biomarkers as substrates for transporter drug‐drug interaction evaluation: perspectives from the international transporter consortium

X Chu, M Liao, H Shen, K Yoshida… - Clinical …, 2018 - Wiley Online Library
Drug transporters can govern the absorption, distribution, metabolism, and excretion of
substrate drugs and endogenous substances. Investigations to examine their potential …

PBPK models for the prediction of in vivo performance of oral dosage forms

ES Kostewicz, L Aarons, M Bergstrand… - European Journal of …, 2014 - Elsevier
Drug absorption from the gastrointestinal (GI) tract is a highly complex process dependent
upon numerous factors including the physicochemical properties of the drug, characteristics …

[HTML][HTML] Renal drug transporters and their significance in drug–drug interactions

J Yin, J Wang - Acta Pharmaceutica Sinica B, 2016 - Elsevier
The kidney is a vital organ for the elimination of therapeutic drugs and their metabolites.
Renal drug transporters, which are primarily located in the renal proximal tubules, play an …

In Vitro Methods to Support Transporter Evaluation in Drug Discovery and Development

KLR Brouwer, D Keppler, KA Hoffmaster… - Clinical …, 2013 - Wiley Online Library
This white paper addresses current approaches and knowledge gaps concerning methods
to assess the role of transport proteins in drug/metabolite disposition in humans. The …

The next frontier in ADME science: Predicting transporter-based drug disposition, tissue concentrations and drug-drug interactions in humans

F Storelli, M Yin, AR Kumar, MK Ladumor… - Pharmacology & …, 2022 - Elsevier
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 …

Protein abundance of clinically relevant drug transporters in the human liver and intestine: a comparative analysis in paired tissue specimens

M Drozdzik, D Busch, J Lapczuk… - Clinical …, 2019 - Wiley Online Library
Bioavailability of orally administered drugs is partly determined by function of drug
transporters in the liver and intestine. Therefore, we explored adenosine triphosphate …

Transporters in drug development: International transporter consortium update on emerging transporters of clinical importance

MJ Zamek‐Gliszczynski, V Sangha… - Clinical …, 2022 - Wiley Online Library
During its fourth transporter workshop in 2021, the International Transporter Consortium
(ITC) provided updates on emerging clinically relevant transporters for drug development …

[HTML][HTML] How drugs get into cells: tested and testable predictions to help discriminate between transporter-mediated uptake and lipoidal bilayer diffusion

DB Kell, SG Oliver - Frontiers in pharmacology, 2014 - frontiersin.org
One approach to experimental science involves creating hypotheses, then testing them by
varying one or more independent variables, and assessing the effects of this variation on the …

Transporters in drug development and clinical pharmacology

KM Giacomini, SM Huang - Clinical Pharmacology & …, 2013 - Wiley Online Library
More than 400 membrane transporters in two major superfamilies—ATP‐binding cassette
(ABC) and solute carrier (SLC)—are annotated in the human genome. Preclinical and …