Interactions of human P-glycoprotein with simvastatin, simvastatin acid, and atorvastatin

JH Hochman, N Pudvah, J Qiu, M Yamazaki… - Pharmaceutical …, 2004 - Springer
Purpose. In this study, P-glycoprotein (P-gp) mediated efflux of simvastatin (SV), simvastatin
acid (SVA), and atorvastatin (AVA) and inhibition of P-gp by SV, SVA, and AVA were …

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 …

The ATP-binding cassette transporters and their implication in drug disposition: a special look at the heart

L Couture, JA Nash, J Turgeon - Pharmacological reviews, 2006 - ASPET
The passage of drugs across cell membranes dictates their absorption, distribution,
metabolism, and excretion. This process is determined by several factors including the …

The physiological function of drug-transporting P-glycoproteins

AH Schinkel - Seminars in cancer biology, 1997 - Elsevier
The mammalian drug-transporting or mdr1-type P-glycoproteins can extrude a range of
structurally diverse, toxic xenobiotic compounds from cells. Our analysis of knockout mice …

Pharmaceutical formulations with P-glycoprotein inhibitory effect as promising approaches for enhancing oral drug absorption and bioavailability

TTL Nguyen, VA Duong, HJ Maeng - Pharmaceutics, 2021 - mdpi.com
P-glycoprotein (P-gp) is crucial in the active transport of various substrates with diverse
structures out of cells, resulting in poor intestinal permeation and limited bioavailability …

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 …

Rapid identification of P-glycoprotein substrates and inhibitors

C Chang, PM Bahadduri, JE Polli, PW Swaan… - Drug metabolism and …, 2006 - ASPET
Identifying molecules that interact with P-glycoprotein (P-gp) is important for drug discovery
but is also generally reliant on time-consuming in vitro and in vivo studies. As an alternative …

The ABCs of drug transport in intestine and liver: efflux proteins limiting drug absorption and bioavailability

LMS Chan, S Lowes, BH Hirst - European journal of pharmaceutical …, 2004 - Elsevier
Many orally administered drugs must overcome several barriers before reaching their target
site. The first major obstacle to cross is the intestinal epithelium. Although lipophilic …

Imaging P‐glycoprotein transport activity at the human blood‐brain barrier with positron emission tomography

L Sasongko, JM Link, M Muzi… - Clinical …, 2005 - Wiley Online Library
Background Numerous knockout mouse studies have revealed that P‐glycoprotein (P‐gp)
significantly limits drug distribution across the mouse blood‐brain barrier (BBB). To …

Structures of the Multidrug Transporter P-glycoprotein Reveal Asymmetric ATP Binding and the Mechanism of Polyspecificity*♦

L Esser, F Zhou, KM Pluchino, J Shiloach, J Ma… - Journal of Biological …, 2017 - ASBMB
P-glycoprotein (P-gp) is a polyspecific ATP-dependent transporter linked to multidrug
resistance in cancer; it plays important roles in determining the pharmacokinetics of many …