In vitro evaluation of hepatic transporter-mediated clinical drug-drug interactions: hepatocyte model optimization and retrospective investigation

Y Bi, E Kimoto, S Sevidal, HM Jones, HA Barton… - Drug Metabolism and …, 2012 - ASPET
To assess the feasibility of using sandwich-cultured human hepatocytes (SCHHs) as a
model to characterize transport kinetics for in vivo pharmacokinetic prediction, the …

Prediction of pharmacokinetics and drug–drug interactions when hepatic transporters are involved

R Li, HA Barton, MV Varma - Clinical pharmacokinetics, 2014 - Springer
Hepatobiliary transport mechanisms have been identified to play a significant role in
determining the systemic clearance for a number of widely prescribed drugs and an …

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 …

Predicting human hepatic clearance from in vitro drug metabolism and transport data: a scientific and pharmaceutical perspective for assessing drug–drug …

G Camenisch, K Umehara - Biopharmaceutics & drug …, 2012 - Wiley Online Library
Objectives Membrane transporters and metabolism are major determinants of the
hepatobiliary elimination of drugs. This work investigates several key questions for drug …

Model-based approaches to predict drug–drug interactions associated with hepatic uptake transporters: preclinical, clinical and beyond

HA Barton, Y Lai, TC Goosen, HM Jones… - Expert opinion on …, 2013 - Taylor & Francis
Introduction: Membrane transporters have been recognized to play a key role in determining
the absorption, distribution and elimination processes of drugs. The organic anion …

Hepatic transporter drug-drug interactions: an evaluation of approaches and methodologies

B Williamson, RJ Riley - Expert Opinion on Drug Metabolism & …, 2017 - Taylor & Francis
ABSTRACT Introduction: Drug-drug interactions (DDIs) continue to account for 5% of
hospital admissions and therefore remain a major regulatory concern. Effective, quantitative …

Comparison of uptake transporter functions in hepatocytes in different species to determine the optimal model for evaluating drug transporter activities in humans

M Liao, Q Zhu, A Zhu, C Gemski, B Ma, E Guan, AP Li… - Xenobiotica, 2019 - Taylor & Francis
A thorough understanding of species-dependent differences in hepatic uptake transporters
is critical for predicting human pharmacokinetics (PKs) from preclinical data. In this study, the …

Quantitative prediction of OATP-mediated disposition and biliary clearance using human liver chimeric mice

T Miyake, H Tsutsui, M Hirabayashi… - Journal of Pharmacology …, 2023 - ASPET
Drug biliary clearance (CLbile) in vivo is among the most difficult pharmacokinetic
parameters to predict accurately and quantitatively because biliary excretion is influenced by …

Impact of hepatic uptake transporters on pharmacokinetics and drug− drug interactions: use of assays and models for decision making in the pharmaceutical industry

MG Soars, PJH Webborn, RJ Riley - Molecular pharmaceutics, 2009 - ACS Publications
The ability to predict hepatic metabolic clearance is a key component in the design and
selection of small molecule drug candidates within the pharmaceutical industry. The …

Reliable rate measurements for active and passive hepatic uptake using plated human hepatocytes

Y Bi, RJ Scialis, S Lazzaro, S Mathialagan, E Kimoto… - The AAPS journal, 2017 - Springer
Transporter-mediated hepatic uptake is proven to be the rate-determining step in the
systemic clearance of several drugs. Therefore, accurate measurement of active and …