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. The overall aim of our study was to investigate the …
drug–drug interactions (DDIs) in vivo. The overall aim of our study was to investigate the …
Application of permeability-limited physiologically-based pharmacokinetic models: part I–digoxin pharmacokinetics incorporating P-glycoprotein-mediated efflux
A prerequisite for the prediction of the magnitude of P-glycoprotein (P-gp)-mediated drug–
drug interactions between digoxin and P-gp inhibitors (eg verapamil and its metabolite …
drug interactions between digoxin and P-gp inhibitors (eg verapamil and its metabolite …
Comparison of P-glycoprotein-mediated drug–digoxin interactions in Caco-2 with human and rodent intestine: Relevance to in vivo prediction
A Collett, J Tanianis-Hughes, GL Carlson… - European journal of …, 2005 - Elsevier
Inhibition of P-glycoprotein (PGP) resulting from the co-administration of substrate drugs
represents a potential source of drug–drug interactions. Although in vitro screens can readily …
represents a potential source of drug–drug interactions. Although in vitro screens can readily …
The utility of in vitro data in making accurate predictions of human P-glycoprotein-mediated drug-drug interactions: a case study for AZD5672
R Elsby, M Gillen, C Butters, G Imisson… - Drug metabolism and …, 2011 - ASPET
To support drug development and registration, Caco-2 cell monolayer assays have
previously been set up and validated to determine whether candidate drugs are substrates …
previously been set up and validated to determine whether candidate drugs are substrates …
Development, validation and utility of an in vitro technique for assessment of potential clinical drug–drug interactions involving P-glycoprotein
JP Keogh, JR Kunta - European journal of pharmaceutical sciences, 2006 - Elsevier
Regulatory interest is increasing for drug transporters generally and P-glycoprotein (Pgp) in
particular, primarily in the area of drug–drug interactions. To aid in both identifying and …
particular, primarily in the area of drug–drug interactions. To aid in both identifying and …
Influence of passive permeability on apparent P-glycoprotein kinetics
KA Lentz, JW Polli, SA Wring, JE Humphreys… - Pharmaceutical …, 2000 - Springer
Purpose. The objectives of this work were to evaluate the importance of moderate passive
permeability on apparent P-glycoprotein (P-gp) kinetics, and demonstrate that inspection of …
permeability on apparent P-glycoprotein (P-gp) kinetics, and demonstrate that inspection of …
Physiologically‐based pharmacokinetic modeling to evaluate in vitro‐to‐in vivo extrapolation for intestinal P‐glycoprotein inhibition
S Yamazaki, R Evers, L De Zwart - CPT: Pharmacometrics & …, 2022 - Wiley Online Library
As one of the key components in model‐informed drug discovery and development,
physiologically‐based pharmacokinetic (PBPK) modeling linked with in vitro‐to‐in vivo …
physiologically‐based pharmacokinetic (PBPK) modeling linked with in vitro‐to‐in vivo …
Substrate-and species-dependent inhibition of P-glycoprotein-mediated transport: implications for predicting in vivo drug interactions
JK Zolnerciks, CL Booth‐Genthe, A Gupta… - Journal of …, 2011 - Elsevier
ABSTRACT P‐glycoprotein (P‐gp)‐based drug interactions are a major concern in the clinic
and in preclinical drug development, especially with respect to the intestinal absorption of …
and in preclinical drug development, especially with respect to the intestinal absorption of …
Challenges of Using In Vitro Data for Modeling P-Glycoprotein Efflux in the Blood-Brain Barrier
N Sjöstedt, H Kortejärvi, H Kidron, KS Vellonen… - Pharmaceutical …, 2014 - Springer
The efficacy of central nervous system (CNS) drugs may be limited by their poor ability to
cross the blood-brain barrier (BBB). Transporters, such as p-glycoprotein, may affect the …
cross the blood-brain barrier (BBB). Transporters, such as p-glycoprotein, may affect the …
Assessing drug distribution in tissues expressing P-glycoprotein through physiologically based pharmacokinetic modeling: model structure and parameters …
F Fenneteau, J Turgeon, L Couture, V Michaud… - Theoretical Biology and …, 2009 - Springer
Background The expression and activity of P-glycoproteins due to genetic or environmental
factors may have a significant impact on drug disposition, drug effectiveness or drug toxicity …
factors may have a significant impact on drug disposition, drug effectiveness or drug toxicity …