Breast Cancer Resistance Protein Abundance, but Not mRNA Expression, Correlates with Estron e-3-Sulfate Transport in Caco-2
Transporter mRNA and protein expression data are used to extrapolate in vitro transporter kinetics to in…
webdev2016 年 4 月 1 日
In Vitro-In Vivo Extrapolation Scaling Factors for Intestinal P-glycoprotein and Breast Cancer Resistance Protein: Part II—The Impact of Cross-laboratory Variations of Intestinal Transporter Relative Expression Factors on Predicted Drug Disposition
Relative expression factors (REFs) are used to scale in vitro transporter kinetic data via in vitro-in vivo extrapolation linked to physiologically based pharmacokinetic (IVIVE-PBPK)…
webdev2016 年 3 月 1 日
In Vitro-In Vivo Extrapolation Scaling Factors for Intestinal P-glycoprotein and Breast Cancer Resistance Protein: Part I—A Cross-laboratory Comparison of Transporter-protein Abundances and Relative Expression Factors in Human Intestine and Caco-2 Cells
Over the last 5 years the quantification of transporter-protein absolute abundances has dramatically increased in parallel to the expanded…
webdev2016 年 3 月 1 日
Interplay of Metabolism and Transport in Determining Oral Drug Absorption and Gut Wall Metabolism: A Simulation Assessment Using the “Advanced Dissolution, Absorption, Metabolism (ADAM)” Model
Bioavailability of orally administered drugs can be influenced by a number of factors including release…
webdev2015 年 11 月 1 日
Lost in Centrifugation: Accounting for Transporter Protein Losses in Quantitative Targeted Absolute Proteomics
In drug development, considerable efforts are made to extrapolate from in vitro and preclinical findings…
webdev2014 年 10 月 1 日
Application of a Physiologically-based Pharmacokinetic Model to Predict OATP1B1-related Variability in Pharmacodynamics of Rosuvastatin
Typically, pharmacokinetic-pharmacodynamic (PK/PD) models use plasma concentration as the input that drives the PD model. However, interindividual variability in…
webdev2014 年 7 月 9 日
Application of Permeability-limited Physiologically-based Pharmacokinetic Models: Part II—Prediction of P-glycoprotein Mediated Drug-drug Interactions with Digoxin
Digoxin is the recommended substrate for assessment of P-glycoprotein (P-gp)-mediated drug-drug interactions (DDIs) in vivo.…
webdev2013 年 9 月 1 日
Application of Permeability-limited Physiologically-based Pharmacokinetic Models: Part I—Digoxin Pharmacokinetic Incorporating P-glycoprotein-mediated Efflux
A prerequisite for the prediction of the magnitude of P-glycoprotein (P-gp)-mediated drug-drug interactions between digoxin…
webdev2013 年 9 月 1 日
A Mechanistic Framework for In Vitro-In Vivo Extrapolation of Liver Membrane Transporters: Prediction of Drug-drug Interaction Between Rosuvastatin and Cyclosporine
The interplay between liver metabolizing enzymes and transporters is a complex process involving system-related parameters such as liver blood perfusion…
webdev2013 年 7 月 24 日
