Variability in P-glycoprotein inhibitory potency (IC50) using various in vitro experimental systems: implications for universal digoxin drug-drug interaction risk …
J Bentz, MP O'Connor, D Bednarczyk… - Drug metabolism and …, 2013 - ASPET
A P-glycoprotein (P-gp) IC50 working group was established with 23 participating
pharmaceutical and contract research laboratories and one academic institution to assess …
pharmaceutical and contract research laboratories and one academic institution to assess …
Refining the In Vitro and In Vivo Critical Parameters for P-Glycoprotein, [I]/IC50 and [I2]/IC50, That Allow for the Exclusion of Drug Candidates from Clinical Digoxin …
JA Cook, B Feng, KS Fenner, S Kempshall… - Molecular …, 2010 - ACS Publications
The objective of this work was to further investigate the reasons for disconcordant clinical
digoxin drug interactions (DDIs) particularly for false negative where in vitro data suggests …
digoxin drug interactions (DDIs) particularly for false negative where in vitro data suggests …
Application of receiver operating characteristic analysis to refine the prediction of potential digoxin drug interactions
In the 2012 Food and Drug Administration (FDA) draft guidance on drug-drug interactions
(DDIs), a new molecular entity that inhibits P-glycoprotein (P-gp) may need a clinical DDI …
(DDIs), a new molecular entity that inhibits P-glycoprotein (P-gp) may need a clinical DDI …
Establishment of in vitro P-glycoprotein inhibition assay and its exclusion criteria to assess the risk of drug–drug interaction at the drug discovery stage
H Sugimoto, SI Matsumoto, M Tachibana… - Journal of …, 2011 - Elsevier
The decision tree to determine whether the P-glycoprotein (P-gp)/multidrug resistance
protein 1 (MDR1)-mediated drug–drug interaction (DDI) study is recommended has been …
protein 1 (MDR1)-mediated drug–drug interaction (DDI) study is recommended has been …
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 …
Drug–Drug Interactions Mediated Through P‐Glycoprotein: Clinical Relevance and In Vitro–In Vivo Correlation Using Digoxin as a Probe Drug
KS Fenner, MD Troutman, S Kempshall… - Clinical …, 2009 - Wiley Online Library
The clinical pharmacokinetics and in vitro inhibition of digoxin were examined to predict the
P‐glycoprotein (P‐gp) component of drug–drug interactions. Coadministered drugs (co …
P‐glycoprotein (P‐gp) component of drug–drug interactions. Coadministered drugs (co …
In vitro p-glycoprotein inhibition assays for assessment of clinical drug interaction potential of new drug candidates: a recommendation for probe substrates
J Rautio, JE Humphreys, LO Webster… - Drug metabolism and …, 2006 - ASPET
Because modulation of P-glycoprotein (Pgp) through inhibition or induction can lead to drug-
drug interactions by altering intestinal, central nervous system, renal, or biliary efflux, it is …
drug interactions by altering intestinal, central nervous system, renal, or biliary efflux, it is …
Determining P-glycoprotein–drug interactions: evaluation of reconstituted P-glycoprotein in a liposomal system and LLC-MDR1 polarized cell monolayers
INTRODUCTION: P-Glycoprotein (ABCB1, MDR1) is a multidrug efflux pump that is a
member of the ATP-binding cassette (ABC) superfamily. Many drugs in common clinical use …
member of the ATP-binding cassette (ABC) superfamily. Many drugs in common clinical use …
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 …
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 …