Design, data analysis, and simulation of in vitro drug transport kinetic experiments using a mechanistic in vitro model
A Poirier, T Lave, R Portmann, ME Brun… - Drug metabolism and …, 2008 - ASPET
The use of in vitro data for quantitative predictions of transporter-mediated elimination in vivo
requires an accurate estimation of the transporter Michaelis-Menten parameters, V max and …
requires an accurate estimation of the transporter Michaelis-Menten parameters, V max and …
In vitro–in vivo extrapolation of hepatic clearance involving active uptake: Theoretical and experimental aspects
PJH Webborn, AJ Parker, RL Denton, RJ Riley - Xenobiotica, 2007 - Taylor & Francis
The importance of hepatic uptake transporters in drug clearance is well recognized. The
subject is reviewed with the intention of providing an overview of the concepts in order to link …
subject is reviewed with the intention of providing an overview of the concepts in order to link …
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 …
exist in vitro, confounding in vitro-in vivo extrapolation. The uptake kinetics of seven organic …
Rationalizing underprediction of drug clearance from enzyme and transporter kinetic data: from in vitro tools to mechanistic modeling
A Galetin - Enzyme kinetics in drug metabolism: fundamentals and …, 2014 - Springer
Over the years, there has been an increase in the number and quality of available in vitro
tools for the assessment of clearance. Complexity of data analysis and modelling of …
tools for the assessment of clearance. Complexity of data analysis and modelling of …
Prediction of the hepatic and renal clearance of transporter substrates in rats using in vitro uptake experiments
T Watanabe, K Maeda, T Kondo, H Nakayama… - Drug metabolism and …, 2009 - ASPET
The clearance route and the absolute values for hepatic and renal clearance of drugs are
important criteria for the selection of drug candidates. Based on pharmacokinetic theory, by …
important criteria for the selection of drug candidates. Based on pharmacokinetic theory, 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 …
selection of small molecule drug candidates within the pharmaceutical industry. The …
Simulations of the nonlinear dose dependence for substrates of influx and efflux transporters in the human intestine
MB Bolger, V Lukacova, WS Woltosz - The AAPS journal, 2009 - Springer
The purpose of this study was to develop simulation and modeling methods for the
evaluation of pharmacokinetics when intestinal influx and efflux transporters are involved in …
evaluation of pharmacokinetics when intestinal influx and efflux transporters are involved in …
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 …
hepatobiliary elimination of drugs. This work investigates several key questions for drug …
Recent progresses in the experimental methods and evaluation strategies of transporter functions for the prediction of the pharmacokinetics in humans
S Kitamura, K Maeda, Y Sugiyama - Naunyn-Schmiedeberg's archives of …, 2008 - Springer
Establishing the methods for the effective screening of compounds with optimal
pharmacokinetic properties is of great importance to many scientists working in new drug …
pharmacokinetic properties is of great importance to many scientists working in new drug …
Absolute abundance and function of intestinal drug transporters: a prerequisite for fully mechanistic in vitro–in vivo extrapolation of oral drug absorption
MD Harwood, S Neuhoff, GL Carlson… - … & drug disposition, 2013 - Wiley Online Library
The use of whole body physiological‐based pharmacokinetic (PBPK) models linked with in
vitro‐in vivo extrapolation (IVIVE) of kinetic parameters from laboratory experiments, has …
vitro‐in vivo extrapolation (IVIVE) of kinetic parameters from laboratory experiments, has …