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Regulation of BCRP (ABCG2) and P-Glycoprotein (ABCB1) by Cytokines in a Model of the Human Blood–Brain Barrier
Brain capillary endothelial cells form the blood–brain barrier (BBB), a highly selective permeability membrane between the blood and the brain. Besides tight junctions that prevent small hydrophilicExpand
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The human brain endothelial cell line hCMEC/D3 as a human blood‐brain barrier model for drug transport studies
The human brain endothelial capillary cell line hCMEC/D3 has been developed recently as a model for the human blood‐brain barrier. In this study a further characterization of this model was performedExpand
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Brain accumulation of sunitinib is restricted by P‐glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by oral elacridar and sunitinib coadministration
Sunitinib is an orally active, multitargeted tyrosine kinase inhibitor which has been used for the treatment of metastatic renal cell carcinoma and imatinib‐resistant gastrointestinal stromal tumors.Expand
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Prediction of Organic Anion-Transporting Polypeptide 1B1- and 1B3-Mediated Hepatic Uptake of Statins Based on Transporter Protein Expression and Activity Data
Organic anion-transporting polypeptides (OATP) 1B1 and OATP1B3 are drug transporters mediating the active hepatic uptake of their substrates. Because they exhibit overlapping substrate specificities,Expand
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Oral administration of glucagon-like peptide 1 or peptide YY 3-36 affects food intake in healthy male subjects.
BACKGROUND Peripheral infusion of glucagon-like peptide 1 (GLP-1) or peptide YY 3-36 (PYY3-36) reduces food intake in healthy, obese, and diabetic subjects. In vivo, both peptides are cosecreted fromExpand
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Differential Impact of P-Glycoprotein (ABCB1) and Breast Cancer Resistance Protein (ABCG2) on Axitinib Brain Accumulation and Oral Plasma Pharmacokinetics
The second-generation tyrosine kinase inhibitor and anticancer drug axitinib is a potent, orally active inhibitor of the vascular endothelial growth factor receptors 1, 2, and 3. Axitinib hasExpand
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In vitro-in vivo extrapolation method to predict human renal clearance of drugs.
Renal clearance is a key determinant of the elimination of drugs. To date, only few in vitro-in vivo extrapolation (IVIVE) approaches have been described to predict the renal organ clearance as theExpand
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Double-transduced MDCKII cells to study human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) interplay in drug transport across the blood-brain barrier.
P-glycoprotein (P-gp/ABCB1) and breast cancer resistance protein (BCRP/ABCG2) combination knockout mice display disproportionately increased brain penetration of shared substrates, includingExpand
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Hypericum perforatum: which constituents may induce intestinal MDR1 and CYP3A4 mRNA expression?
In vitro and in vivo studies suggest that extracts of St John's wort (Hypericum perforatum, L .; SJWE) interact with various drugs, by enhancing their elimination, due to induction of intestinal andExpand
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Application of the extended clearance concept classification system (ECCCS) to predict the victim drug-drug interaction potential of statins
Abstract Background: During drug development, it is an important safety factor to identify the potential of new molecular entities to become a victim of drug-drug interactions (DDIs). In preclinicalExpand
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