Quantitative contribution of six major transporters to the hepatic uptake of drugs:“SLC-phenotyping” using primary human hepatocytes

Y Bi, C Costales, S Mathialagan, M West… - … of Pharmacology and …, 2019 - ASPET
Hepatic uptake transporters [solute carriers (SLCs)], including organic anion transporting
polypeptide (OATP) 1B1, OATP1B3, OATP2B1, sodium-dependent taurocholate …

Intracellular drug concentrations and transporters: measurement, modeling, and implications for the liver

X Chu, K Korzekwa, R Elsby, K Fenner… - Clinical …, 2013 - Wiley Online Library
Intracellular concentrations of drugs and metabolites are often important determinants of
efficacy, toxicity, and drug interactions. Hepatic drug distribution can be affected by many …

Interplay of drug-metabolizing enzymes and transporters in drug absorption and disposition

S Shi, Y Li - Current drug metabolism, 2014 - ingentaconnect.com
In recent years, the functional interplay between drug-metabolizing enzymes (DMEs) and
drug transporters (DTs) in drug absorption and disposition, as well as the complex drug …

Impact of genetic variation in OATP transporters to drug disposition and response

IY Gong, RB Kim - Drug metabolism and pharmacokinetics, 2013 - jstage.jst.go.jp
There has been remarkable progress during the past decade in understanding of how
genetic variations in drug metabolizing enzymes and transporters contribute to observed …

Interplay of drug metabolism and transport: a real phenomenon or an artifact of the site of measurement?

CJ Endres, MG Endres, JD Unadkat - Molecular pharmaceutics, 2009 - ACS Publications
The interdependence of both transport and metabolism on the disposition of drugs has
recently gained heightened attention in the literature, and has been termed the “interplay of …

Scientific and regulatory perspectives on metabolizing enzyme− transporter interplay and its role in drug interactions: challenges in predicting drug interactions

L Zhang, Y Zhang, SM Huang - Molecular pharmaceutics, 2009 - ACS Publications
Both metabolizing enzymes and drug transporters play important roles in modulating drug
absorption, distribution, metabolism and elimination. Acting alone or in concert with each …

[HTML][HTML] Quantitative prediction of pharmacokinetic properties of drugs in humans: Recent advance in in vitro models to predict the impact of efflux transporters in the …

Y Hashimoto, K Michiba, K Maeda… - Journal of Pharmacological …, 2022 - Elsevier
Efflux transport systems are essential to suppress the absorption of xenobiotics from the
intestinal lumen and protect the critical tissues at the blood-tissue barriers, such as the blood …

Organic anion transporting polypeptide 2B1–more than a glass-full of drug interactions

SJ McFeely, L Wu, TK Ritchie, J Unadkat - Pharmacology & therapeutics, 2019 - Elsevier
The importance of uptake transporters in determining drug disposition is increasingly
appreciated. While the focus of regulatory agencies worldwide has been on the hepatic …

Use of mechanistic modeling to assess interindividual variability and interspecies differences in active uptake in human and rat hepatocytes

K Menochet, KE Kenworthy, JB Houston… - Drug Metabolism and …, 2012 - ASPET
Interindividual variability in activity of uptake transporters is evident in vivo, yet limited data
exist in vitro, confounding in vitro-in vivo extrapolation. The uptake kinetics of seven organic …

A clinical cassette dosing study for evaluating the contribution of hepatic OATPs and CYP3A to drug-drug interactions

T Yoshikado, K Maeda, S Furihata, H Terashima… - Pharmaceutical …, 2017 - Springer
Purpose To demonstrate the relative importance of organic anion-transporting polypeptides
(OATPs) and cytochrome P450 3A (CYP3A) in the hepatic elimination of substrate drugs …