Search Results - "Poller, Birk"
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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
Published in Drug metabolism and disposition (01-09-2014)“…Organic anion-transporting polypeptides (OATP) 1B1 and OATP1B3 are drug transporters mediating the active hepatic uptake of their substrates. Because they…”
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A Systematic In Vitro Investigation of the Inhibitor Preincubation Effect on Multiple Classes of Clinically Relevant Transporters
Published in Drug metabolism and disposition (01-07-2019)“…Preincubation of a drug transporter with its inhibitor in a cell-based assay may result in the apparent enhancement of the inhibitory potency. Currently,…”
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human brain endothelial cell line hCMEC/D3 as a human blood-brain barrier model for drug transport studies
Published in Journal of neurochemistry (01-12-2008)“…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…”
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4
The application of organ-on-chip models for the prediction of human pharmacokinetic profiles during drug development
Published in Pharmacological research (01-09-2023)“…Organ-on-chip (OoC) technology has led to in vitro models with many new possibilities compared to conventional in vitro and in vivo models. In this review, the…”
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5
Regulation of BCRP (ABCG2) and P-Glycoprotein (ABCB1) by Cytokines in a Model of the Human Blood-Brain Barrier
Published in Cellular and molecular neurobiology (01-01-2010)“…Brain capillary endothelial cells form the blood-brain barrier (BBB), a highly selective permeability membrane between the blood and the brain. Besides tight…”
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6
In vitro-in vivo extrapolation method to predict human renal clearance of drugs
Published in Journal of pharmaceutical sciences (01-03-2014)“…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…”
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New IVIVE method for the prediction of total human clearance and relative elimination pathway contributions from in vitro hepatocyte and microsome data
Published in European journal of pharmaceutical sciences (30-04-2016)“…Total human clearance is a key determinant for the pharmacokinetic behavior of drug candidates. Our group recently introduced the Extended Clearance Model…”
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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
Published in Molecular pharmaceutics (04-04-2011)“…P-glycoprotein (P-gp/ABCB1) and breast cancer resistance protein (BCRP/ABCG2) combination knockout mice display disproportionately increased brain penetration…”
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Novel Bruton’s Tyrosine Kinase inhibitor remibrutinib: Drug‐drug interaction potential as a victim of CYP3A4 inhibitors based on clinical data and PBPK modeling
Published in Clinical and translational science (01-01-2022)“…Remibrutinib, a novel oral Bruton’s Tyrosine Kinase inhibitor (BTKi) is highly selective for BTK, potentially mitigating the side effects of other BTKis…”
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10
LTA4H inhibitor LYS006: Clinical PK/PD and safety in a randomized phase I clinical trial
Published in Clinical and translational science (01-02-2024)“…LYS006 is a novel, highly potent and selective, new‐generation leukotriene A4 hydrolase (LTA4H) inhibitor in clinical development for the treatment of…”
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Differential Impact of P-Glycoprotein (ABCB1) and Breast Cancer Resistance Protein (ABCG2) on Axitinib Brain Accumulation and Oral Plasma Pharmacokinetics
Published in Drug metabolism and disposition (01-05-2011)“…The second-generation tyrosine kinase inhibitor and anticancer drug axitinib is a potent, orally active inhibitor of the vascular endothelial growth factor…”
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Cytokine signaling in the human brain capillary endothelial cell line hCMEC/D3
Published in Brain research (01-10-2010)“…Abstract Brain microvascular endothelial cells are part of the blood–brain barrier and participate actively in immunological processes including…”
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Simplifying the Extended Clearance Concept Classification System (EC3S) to Guide Clearance Prediction in Drug Discovery
Published in Pharmaceutical research (01-04-2023)“…Purpose The Extended Clearance Concept Classification System was established as a development-stage tool to provide a framework for identifying fundamental…”
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Improving In Vitro-In Vivo Extrapolation (IVIVE) of Clearance Using Rat Liver Microsomes for Highly Plasma Protein Bound Molecules
Published in Drug metabolism and disposition (01-05-2024)“…It is common practice in drug discovery and development to predict in vivo hepatic clearance from in vitro incubations with liver microsomes or hepatocytes…”
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15
Assessing the Risk of Drug-Induced Cholestasis Using Unbound Intrahepatic Concentrations
Published in Drug metabolism and disposition (01-05-2017)“…Inhibition of the bile salt export pump (BSEP) has been recognized as a key factor in the development of drug-induced cholestasis (DIC). The risk of DIC in…”
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Clinical Investigation of Metabolic and Renal Clearance Pathways Contributing to the Elimination of Fevipiprant Using Probenecid as Perpetrator
Published in Drug metabolism and disposition (01-05-2021)“…Fevipiprant, an oral, nonsteroidal, highly selective, reversible, and competitive prostaglandin D receptor 2 antagonist, is eliminated by glucuronidation and…”
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Drug-induced cholestasis (DIC) predictions based on in vitro inhibition of major bile acid clearance mechanisms
Published in Archives of toxicology (14-11-2024)“…Drug-induced cholestasis (DIC) is recognized as a major safety concern in drug development, as it represents one of the three types of drug-induced liver…”
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Absorption, Distribution, Metabolism, and Excretion of [ 14 C]iptacopan in Healthy Male Volunteers and in In Vivo and In Vitro Studies
Published in Drug metabolism and disposition (01-07-2023)“…Iptacopan (LNP023) is an oral, small-molecule, first-in-class, highly potent proximal complement inhibitor that specifically binds factor B and inhibits the…”
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The extended clearance model and its use for the interpretation of hepatobiliary elimination data
Published in ADMET & DMPK (31-03-2015)“…Hepatic elimination is a function of the interplay between different processes such as sinusoidal uptake, intracellular metabolism, canalicular (biliary)…”
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Novel insights into bile acid detoxification via CYP, UGT and SULT enzymes
Published in Toxicology in vitro (01-03-2023)“…Bile acid (BA) homeostasis is a complex and precisely regulated process to prevent impaired BA flow and the development of cholestasis. Several reactions,…”
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