Species differences in drug transporters and implications for translating preclinical findings to humans
X Chu, K Bleasby, R Evers - Expert opinion on drug metabolism & …, 2013 - Taylor & Francis
Introduction: Drug transporters play an important role in the absorption, distribution, and
excretion (ADE) of many drugs. In the last several years it has become increasingly clear …
excretion (ADE) of many drugs. In the last several years it has become increasingly clear …
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 …
to assess the role of transport proteins in drug/metabolite disposition in humans. The …
[HTML][HTML] Recent advances in the translation of drug metabolism and pharmacokinetics science for drug discovery and development
Y Lai, X Chu, L Di, W Gao, Y Guo, X Liu, C Lu… - … Pharmaceutica Sinica B, 2022 - Elsevier
Drug metabolism and pharmacokinetics (DMPK) is an important branch of pharmaceutical
sciences. The nature of ADME (absorption, distribution, metabolism, excretion) and PK …
sciences. The nature of ADME (absorption, distribution, metabolism, excretion) and PK …
Mechanistic pharmacokinetic modeling for the prediction of transporter-mediated disposition in humans from sandwich culture human hepatocyte data
With efforts to reduce cytochrome P450-mediated clearance (CL) during the early stages of
drug discovery, transporter-mediated CL mechanisms are becoming more prevalent …
drug discovery, transporter-mediated CL mechanisms are becoming more prevalent …
ITC recommendations for transporter kinetic parameter estimation and translational modeling of transport‐mediated PK and DDIs in humans
MJ Zamek‐Gliszczynski, CA Lee… - Clinical …, 2013 - Wiley Online Library
This white paper provides a critical analysis of methods for estimating transporter kinetics
and recommendations on proper parameter calculation in various experimental systems …
and recommendations on proper parameter calculation in various experimental systems …
Interindividual variability in hepatic organic anion-transporting polypeptides and P-glycoprotein (ABCB1) protein expression: quantification by liquid chromatography …
Interindividual variability in protein expression of organic anion-transporting polypeptides
(OATPs) OATP1B1, OATP1B3, OATP2B1, and multidrug resistance-linked P-glycoprotein (P …
(OATPs) OATP1B1, OATP1B3, OATP2B1, and multidrug resistance-linked P-glycoprotein (P …
[HTML][HTML] How drugs get into cells: tested and testable predictions to help discriminate between transporter-mediated uptake and lipoidal bilayer diffusion
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 …
varying one or more independent variables, and assessing the effects of this variation on the …
Cell cultures in drug discovery and development: The need of reliable in vitro-in vivo extrapolation for pharmacodynamics and pharmacokinetics assessment
For ethical and cost-related reasons, use of animals for the assessment of mode of action,
metabolism and/or toxicity of new drug candidates has been increasingly scrutinized in …
metabolism and/or toxicity of new drug candidates has been increasingly scrutinized in …
The promiscuous binding of pharmaceutical drugs and their transporter-mediated uptake into cells: what we (need to) know and how we can do so
A recent paper in this journal sought to counter evidence for the role of transport proteins in
effecting drug uptake into cells, and questions that transporters can recognize drug …
effecting drug uptake into cells, and questions that transporters can recognize drug …
Prediction of organic anion-transporting polypeptide 1B1-and 1B3-mediated hepatic uptake of statins based on transporter protein expression and activity data
A Kunze, J Huwyler, G Camenisch, B Poller - Drug Metabolism and …, 2014 - ASPET
Organic anion-transporting polypeptides (OATP) 1B1 and OATP1B3 are drug transporters
mediating the active hepatic uptake of their substrates. Because they exhibit overlapping …
mediating the active hepatic uptake of their substrates. Because they exhibit overlapping …