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 …
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 …
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 …
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 …
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
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 …
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 …
active metabolite, and seven non-CNS-active compounds were tested in three P …
Rapid identification of P-glycoprotein substrates and inhibitors
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 …
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
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 …
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
Background Numerous knockout mouse studies have revealed that P‐glycoprotein (P‐gp)
significantly limits drug distribution across the mouse blood‐brain barrier (BBB). To …
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*♦
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 …
resistance in cancer; it plays important roles in determining the pharmacokinetics of many …