Does inhibition of P-glycoprotein lead to drug–drug interactions?

D Balayssac, N Authier, A Cayre, F Coudore - Toxicology letters, 2005 - Elsevier
Permeability-glycoprotein (Pgp) is a drug transporter responsible for the efflux of xenobiotics
out of cells that influence the pharmacokinetics of numerous drugs. However, the role of this …

Transport of digoxin by human P-glycoprotein expressed in a porcine kidney epithelial cell line (LLC-PK1).

Y Tanigawara, N Okamura, M Hirai, M Yasuhara… - … of Pharmacology and …, 1992 - ASPET
This article represents the first evidence that the renal secretion of the commonly used drug,
digoxin, is mediated by P-glycoprotein. In this study, it was demonstrated that digoxin is a …

Drug–drug interaction mediated by inhibition and induction of P-glycoprotein

JH Lin - Advanced drug delivery reviews, 2003 - Elsevier
P-glycoprotein (P-gp), the most extensively studied ATP-binding cassette transporter,
functions as a biological barrier by extruding toxic substances and xenobiotics out of cells. In …

Computational models for identifying potential P-glycoprotein substrates and inhibitors

P Crivori, B Reinach, D Pezzetta… - Molecular …, 2006 - ACS Publications
Multidrug resistance mediated by ATP binding cassette (ABC) transporters such as P-
glycoprotein (P-gp) represents a serious problem for the development of effective anticancer …

Evidence for a non-MDR1 component in digoxin secretion by human intestinal Caco-2 epithelial layers

S Lowes, ME Cavet, NL Simmons - European journal of pharmacology, 2003 - Elsevier
Caco-2 epithelial layers were used as a model to re-evaluate the mechanism (s) by which
intestinal digoxin absorption is limited by its active secretion back into the lumen. It is widely …

Toxic digoxin-drug interactions: the major role of renal P-glycoprotein.

G Koren, C Woodland, S Ito - Veterinary and human toxicology, 1998 - europepmc.org
The clinical use of digoxin is complicated by a large number of drug interactions leading to
severe toxicity of the cardiac glycoside. The discovery that digoxin is actively secreted by the …

In vitro P-glycoprotein efflux ratio can predict the in vivo brain penetration regardless of biopharmaceutics drug disposition classification system class

R Kikuchi, SM de Morais, JC Kalvass - Drug Metabolism and Disposition, 2013 - ASPET
P-glycoprotein (P-gp) is expressed at the blood-brain barrier (BBB) and restricts the
penetration of its substrates into the central nervous system (CNS). In vitro substrate …

Predicting P-glycoprotein substrates by a quantitative structure–activity relationship model

VK Gombar, JW Polli, JE Humphreys, SA Wring… - Journal of …, 2004 - Elsevier
A quantitative structure–activity relationship (QSAR) model has been developed to predict
whether a given compound is a P‐glycoprotein (Pgp) substrate or not. The training set …

Meta‐analysis of the influence of MDR1 C3435T polymorphism on digoxin pharmacokinetics and MDR1 gene expression

B Chowbay, H Li, M David… - British journal of …, 2005 - Wiley Online Library
Aims Studies revealing conflicting results of the functional significance of MDR1 exon 26
C3435T SNP on the disposition of digoxin in different ethnic groups led us to perform a meta …

Clinical relevance of hepatic and renal P‐gp/BCRP inhibition of drugs: An international transporter consortium perspective

KS Taskar, X Yang, S Neuhoff, M Patel… - Clinical …, 2022 - Wiley Online Library
The role of P‐glycoprotein (P‐gp) and breast cancer resistance protein (BCRP) in drug–drug
interactions (DDIs) and limiting drug absorption as well as restricting the brain penetration of …