Role of P-Glycoprotein and Organic Anion Transporting Polypeptides in Drug Absorption and Distribution: Focus on H1-Receptor Antagonists

PD Hansten, RH Levy - Clinical Drug Investigation, 2001 - Springer
Traditionally, drug-induced changes in cytochrome P450 isoenzyme activity, causing
changes in drug metabolism and bioavailability, have been the main focus of drug …

Effect of P‐glycoprotein expression levels on the concentration‐dependent permeability of drugs to the cell membrane

Y Shirasaka, T Sakane, S Yamashita - Journal of pharmaceutical sciences, 2008 - Elsevier
The purpose of this study is to develop a kinetic model that can predict the in vivo absorption
of P‐glycoprotein (P‐gp) substrates from in vitro data. Apical (AP) to basal (BL) absorptive …

In vitro P-glycoprotein assays to predict the in vivo interactions of P-glycoprotein with drugs in the central nervous system

B Feng, JB Mills, RE Davidson, RJ Mireles… - Drug Metabolism and …, 2008 - ASPET
Thirty-one structurally diverse marketed central nervous system (CNS)-active drugs, one
active metabolite, and seven non-CNS-active compounds were tested in three P …

Study Models of Drug–Drug Interactions Involving P-Glycoprotein: The Potential Benefit of P-Glycoprotein Modulation at the Kidney and Intestinal Levels

J Veiga-Matos, AI Morales, M Prieto, F Remião, R Silva - Molecules, 2023 - mdpi.com
P-glycoprotein (P-gp) is a crucial membrane transporter situated on the cell's apical surface,
being responsible for eliminating xenobiotics and endobiotics. P-gp modulators are …

Structural and functional aspects of P-glycoprotein and its inhibitors

S Mollazadeh, A Sahebkar, F Hadizadeh, J Behravan… - Life sciences, 2018 - Elsevier
Abstract P-glycoprotein (P-gp) is a member of ATP-binding cassette (ABC) superfamily
which extrudes chemotherapeutic agents out of the cell. Suppression of this efflux activity …

ABCB1 single nucleotide polymorphisms (1236C> T, 2677G> T, and 3435C> T) do not affect transport activity of human P-glycoprotein

D Dickens, A Owen, A Alfirevic… - Pharmacogenetics and …, 2013 - journals.lww.com
Background P-glycoprotein (P-gp) is a multidrug efflux transporter that has a defined role in
the absorption and disposition of drugs. Many studies have investigated the potential …

[PDF][PDF] In vitro P-glycoprotein inhibition assay on N2a murine cell line

AC Nicolae, N Mitrea, AL Arsene… - IN …, 2013 - farmaciajournal.com
Abstract P-glycoprotein (Pgp), also called MDR1, the product of the multidrug resistance
(MDR) gene, is an ATP-dependent efflux transporter that affects the absorption, distribution …

[引用][C] Drug-drug interaction studies of cardiovascular drugs (amiodarone, digoxin, quinidine, atorvastatin and verapamil) involving P-glycoprotein (P-gp), an efflux …

J Mendell, H Zahir, G Ridout, R Noveck, F Lee… - Journal of the American …, 2011 - jacc.org
Background: Edoxaban, an oral direct factor Xa inhibitor, is in phase 3 clinical development
for stroke prevention in AF and treatment of VTE. P-gp, an efflux transporter, can prevent the …

In vitro-to-in vivo prediction of P-glycoprotein-based drug interactions at the human and rodent blood-brain barrier

P Hsiao, T Bui, RJY Ho, JD Unadkat - Drug metabolism and disposition, 2008 - ASPET
In vitro inhibition of P-glycoprotein (P-gp) expressed in cells is routinely used to predict the
potential of in vivo P-gp drug interactions at the human blood-brain barrier (BBB). The …

P-glycoprotein system as a determinant of drug interactions: the case of digoxin–verapamil

M Verschraagen, CHW Koks, JHM Schellens… - Pharmacological …, 1999 - Elsevier
Digoxin, which has a very narrow therapeutic window, is one of the most commonly
prescribed drugs in the treatment of congestive heart failure. In some cases of atrial …