Mechanistic Pharmacokinetic Modeling for the Prediction of Transporter-Mediated Disposition in Humans from Sandwich Culture Human Hepatocyte Data

No abstract is available for this paper.

• Publication year

  2012

• Venue

  Drug Metabolism And Disposition

• Publication date

  2012-05-01

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1124/dmd.111.042994PMID 22344703
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• In Vitro Evaluation of Hepatic Transporter-Mediated Clinical Drug-Drug Interactions: Hepatocyte Model Optimization and Retrospective Investigation

  2012cited by this paper
• Absolute Quantification and Differential Expression of Drug Transporters, Cytochrome P450 Enzymes, and UDP-Glucuronosyltransferases in Cultured Primary Human Hepatocytes

  2012cited by this paper
• Culture Period-Dependent Changes in the Uptake of Transporter Substrates in Sandwich-Cultured Rat and Human Hepatocytes

  2011cited by this paper
• Simulation of Human Intravenous and Oral Pharmacokinetics of 21 Diverse Compounds Using Physiologically Based Pharmacokinetic Modelling

  2011cited by this paper
• Mechanisms Underlying Differences in Systemic Exposure of Structurally Similar Active Metabolites: Comparison of Two Preclinical Hepatic Models

  2011influential reference
• Kinetic Characterization of Rat Hepatic Uptake of 16 Actively Transported Drugs

  2011cited by this paper
• Physiologically Based Pharmacokinetic Modeling of Intestinal First-Pass Metabolism of CYP3A Substrates with High Intestinal Extraction

  2011cited by this paper
• Membrane transporters in drug development

  2010cited by this paper
• Prediction of Human Intestinal First-Pass Metabolism of 25 CYP3A Substrates from In Vitro Clearance and Permeability Data

  2010cited by this paper
• Hepatobiliary Disposition of Troglitazone and Metabolites in Rat and Human Sandwich-Cultured Hepatocytes: Use of Monte Carlo Simulations to Assess the Impact of Changes in Biliary Excretion on Troglitazone Sulfate Accumulation

  2010influential reference
• Improved extrapolation of hepatobiliary clearance from in vitro sandwich cultured rat hepatocytes through absolute quantification of hepatobiliary transporters.

  2010cited by this paper
• Investigation of the Rate-Determining Process in the Hepatic Elimination of HMG-CoA Reductase Inhibitors in Rats and Humans

  2010cited by this paper
• Physiologically Based Pharmacokinetic Modelling

  2009cited by this paper
• Impact of hepatic uptake transporters on pharmacokinetics and drug-drug interactions: use of assays and models for decision making in the pharmaceutical industry.

  2009cited by this paper
• Mechanistic modeling of hepatic transport from cells to whole body: application to napsagatran and fexofenadine.

  2009influential reference
• Physiologically Based Pharmacokinetic Modeling to Predict Transporter-Mediated Clearance and Distribution of Pravastatin in Humans

  2009influential reference
• Prediction of pharmacokinetic profile of valsartan in human based on in vitro uptake transport data

  2009influential reference
• Involvement of Multiple Transporters in the Hepatobiliary Transport of Rosuvastatin

  2008influential reference
• Design, Data Analysis, and Simulation of in Vitro Drug Transport Kinetic Experiments Using a Mechanistic in Vitro Model

  2008influential reference
• Pre-clinical pharmacokinetics of UK-453,061, a novel non-nucleoside reverse transcriptase inhibitor (NNRTI), and use of in silico physiologically based prediction tools to predict the oral pharmacokinetics of UK-453,061 in man.

  2008cited by this paper
• Prediction of the Pharmacokinetics of Atorvastatin, Cerivastatin, and Indomethacin Using Kinetic Models Applied to Isolated Rat Hepatocytes

  2008influential reference
• Prediction of Human Pharmacokinetics Using Physiologically Based Modeling: A Retrospective Analysis of 26 Clinically Tested Drugs

  2007cited by this paper
• Human organic anion transporter 1B1 and 1B3 function as bidirectional carriers and do not mediate GSH-bile acid cotransport.

  2007cited by this paper
• Expression of Thirty-six Drug Transporter Genes in Human Intestine, Liver, Kidney, and Organotypic Cell Lines

  2007cited by this paper
• Simulation and prediction of in vivo drug metabolism in human populations from in vitro data

  2007cited by this paper
• A Novel Strategy for Physiologically Based Predictions of Human Pharmacokinetics

  2006cited by this paper
• INVOLVEMENT OF TRANSPORTERS IN THE HEPATIC UPTAKE AND BILIARY EXCRETION OF VALSARTAN, A SELECTIVE ANTAGONIST OF THE ANGIOTENSIN II AT1-RECEPTOR, IN HUMANS

  2006cited by this paper
• Use of Cryopreserved Human Hepatocytes in Sandwich Culture to Measure Hepatobiliary Transport

  2006cited by this paper
• Biliary secretion of rosuvastatin and bile acids in humans during the absorption phase.

  2006cited by this paper
• An integrated approach to model hepatic drug clearance.

  2006cited by this paper
• Physiologically based pharmacokinetic modelling 2: predicting the tissue distribution of acids, very weak bases, neutrals and zwitterions.

  2006cited by this paper
• Predicting Drug Disposition via Application of BCS: Transport/Absorption/ Elimination Interplay and Development of a Biopharmaceutics Drug Disposition Classification System

  2004influential reference
• Interspecies Scaling of Bosentan, A New Endothelin Receptor Antagonist and Integration of in Vitro Data into Allometric Scaling

  2004cited by this paper
• Absolute oral bioavailability of rosuvastatin in healthy white adult male volunteers.

  2003cited by this paper
• Pharmacokinetics and disposition of rosuvastatin, a new 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, in rat

  2002cited by this paper
• Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver

  2002influential reference
• Uptake of teicoplanin by isolated rat hepatocytes: comparison with in vivo hepatic distribution.

  2001cited by this paper
• A priori prediction of tissue:plasma partition coefficients of drugs to facilitate the use of physiologically-based pharmacokinetic models in drug discovery.

  2000cited by this paper
• Use of Ca2+ modulation to evaluate biliary excretion in sandwich-cultured rat hepatocytes.

  1999cited by this paper
• Use of Ca 2 1 Modulation to Evaluate Biliary Excretion in Sandwich-Cultured Rat Hepatocytes 1

  1999influential reference
• Bioavailability of repaglinide, a novel antidiabetic agent, administered orally in tablet or solution form or intravenously in healthy male volunteers.

  1998cited by this paper
• Physiologically based pharmacokinetics of cyclosporine A: extension to tissue distribution kinetics in rats and scale-up to human.

  1998cited by this paper
• Integration of in vitro data into allometric scaling to predict hepatic metabolic clearance in man: application to 10 extensively metabolized drugs.

  1997cited by this paper
• Absolute and relative bioavailability of the HMG-CoA reductase inhibitor cerivastatin.

  1997cited by this paper
• Absolute bioavailability and pharmacokinetics of valsartan, an angiotensin II receptor antagonist, in man

  1997cited by this paper
• Pharmacokinetics and pharmacodynamics of the endothelin‐receptor antagonist bosentan in healthy human subjects

  1996cited by this paper
• Jejunal permeability and hepatic extraction of fluvastatin in humans

  1996cited by this paper
• Utility of in vitro drug metabolism data in predicting in vivo metabolic clearance.

  1994cited by this paper
• Disposition of pravastatin sodium, a tissue-selective HMG-CoA reductase inhibitor, in healthy subjects.

  1990cited by this paper
• Some fundamental considerations of the applications of pharmacokinetics to cancer chemotherapy.

  1975cited by this paper
• Some fundamental considerations of the applications of pharmacokinetics to cancer chemotherapy.

  1975cited by this paper

• Applications of in vitro transporter assays for mechanistic characterization and prediction of clinical drug-drug interactions.

  2026cites this paper
• Quantitative clinical risk assessment of CYP2C, UDP-glucuronosyltransferase, P-glycoprotein induction, and complex drug-drug interactions using TruVivo human hepatocyte triculture platform.

  2025cites this paper
• Predicting Systemic and Liver Bosentan Exposure Using Physiologically‐Based Pharmacokinetic Modeling

  2025cites this paper
• Characterization of small molecule drug clearance mechanisms using in vitro and in vivo approaches in drug discovery and development

  2025cites this paper
• In silico modeling and simulation of organ‐on‐a‐chip systems to support data analysis and a priori experimental design

  2024cites this paper
• Drug transporters in drug disposition – highlights from the year 2023

  2024cites this paper
• Building a Predictive PBPK Model for Human OATP Substrates: a Strategic Framework for Early Evaluation of Clinical Pharmacokinetic Variations Using Pitavastatin as an Example

  2024cites this paper
• In Vitro-In Vivo Extrapolation and Scaling Factors for Clearance of Human and Preclinical Species with Liver Microsomes and Hepatocytes

  2023cites this paper
• Interpretation of Protein-Mediated Uptake of Statins by Hepatocytes Is Confounded by the Residual Statin-Protein Complex

  2023cites this paper
• The Current Status and Use of Microphysiological Systems by the Pharmaceutical Industry: The International Consortium for Innovation and Quality Microphysiological Systems Affiliate Survey and Commentary

  2023cites this paper
• Utility of Minimal Physiologically Based Pharmacokinetic Models for Assessing Fractional Distribution, Oral Absorption, and Series-Compartment Models of Hepatic Clearance

  2023cites this paper
• A Complete Extension of Classical Hepatic Clearance Models Using Fractional Distribution Parameter fd in Physiologically Based Pharmacokinetics.

  2023cites this paper
• Exploring the Pharmacokinetic Mysteries of the Liver: Application of Series Compartment Models of Hepatic Elimination

  2023cites this paper
• Use of selective substrates and inhibitors to rapidly characterise batches of cryopreserved primary human hepatocytes for assessment of active uptake liability in drug discovery and development

  2022cites this paper
• Predictive performance of next generation human physiologically based kinetic (PBK) model predictions based on in vitro and in silico input data_suppl1

  2022cites this paper
• Current strategies with implementation of three-dimensional cell culture: the challenge of quantification

  2022cites this paper
• Current Approaches for Predicting Human PK for Small Molecule Development Candidates: Findings from the IQ Human PK Prediction Working Group Survey

  2022cites this paper
• Novel insights in drug transporter sciences: the year 2021 in review

  2022cites this paper
• Novel Method for Kinetic Analysis Applied to Transport by the Uniporter, OCT2.

  2022cites this paper
• Evaluation of a Rapid, Generic Human Gestational Dose Model.

  2022cites this paper
• Assessing Liver-to-Plasma Partition Coefficients and In Silico Calculation Methods: When Does the Hepatic Model Matter in PBPK?

  2022cites this paper
• Is the Protein-Mediated Uptake of Drugs by Organic Anion Transporting Polypeptides a Real Phenomenon or an Artifact?

  2022cites this paper
• The impact of reference data selection for the prediction accuracy of intrinsic hepatic metabolic clearance.

  2022cites this paper
• Predictive Performance of Next Generation Human Physiologically Based Kinetic (PBK) Models Based on In Vitro and In Silico Input Data

  2022cites this paper
• The next frontier in ADME science: Predicting transporter-based drug disposition, tissue concentrations and drug-drug interactions in humans.

  2022cites this paper
• Towards best use and regulatory acceptance of generic physiologically based kinetic (PBK) models for in vitro-to-in vivo extrapolation (IVIVE) in chemical risk assessment

  2022cites this paper
• 3D bioprinted organ‐on‐chips

  2022cites this paper
• Analysis of Time-Dependent Pharmacokinetics Using In Vitro–In Vivo Extrapolation and Physiologically Based Pharmacokinetic Modeling

  2022cites this paper
• Prediction of Hepatobiliary Clearances and Hepatic Concentrations of Transported Drugs in Humans Using Rosuvastatin as a Model Drug

  2022cites this paper
• Going with the Flow: Modeling the Tumor Microenvironment Using Microfluidic Technology

  2021cites this paper
• High-throughput PBTK models for in vitro to in vivo extrapolation

  2021cites this paper
• Application of a PBPK model to elucidate the changes of systemic and liver exposures for rosuvastatin, carotegrast, and bromfenac followed by OATP inhibition in monkeys

  2021cites this paper
• UPLC-MS/MS method for the simultaneous quantification of pravastatin, fexofenadine, rosuvastatin and methotrexate in a hepatic uptake model and it's application to the possible drug-drug-interaction study of triptolide.

  2021cites this paper
• Evolving approaches on measurements and applications of intracellular free drug concentration and Kpuu in drug discovery

  2021cites this paper
• Overcoming the shortcomings of the extended-clearance concept: a framework for developing a physiologically-based pharmacokinetic (PBPK) model to select drug candidates involving transporter-mediated clearance

  2021cites this paper
• OATP1B1/1B3-mediated hepatic uptake determines the pharmacokinetics of large lipophilic acids: In vitro–in vivo evaluation in cynomolgus monkey

  2021cites this paper
• Hepatic transporter‐mediated pharmacokinetic drug–drug interactions: Recent studies and regulatory recommendations

  2021cites this paper
• Improving the Translation of Organic Anion Transporting Polypeptide Substrates using HEK293 Cell Data in the Presence and Absence of Human Plasma via Physiologically Based Pharmacokinetic Modeling

  2021influential citation
• Physiologically Based Pharmacokinetic Modeling of Rosuvastatin to Predict Transporter-Mediated Drug-Drug Interactions

  2021cites this paper
• GUIDANCE DOCUMENT ON THE CHARACTERISATION, VALIDATION AND REPORTING OF PBK MODELS FOR REGULATORY PURPOSES

  2021cites this paper
• Organic Anion–Transporting Polypeptide 1B1/1B3–Mediated Hepatic Uptake Determines the Pharmacokinetics of Large Lipophilic Acids: In Vitro–In Vivo Evaluation in Cynomolgus Monkey

  2021cites this paper
• Mechanism‐Based Experimental Models for the Evaluation of BSEP Inhibition and DILI

  2021cites this paper
• Advancing Estimation of Hepatobiliary Clearances in Physiologically Based Pharmacokinetic Models of Rosuvastatin Using Human Hepatic Concentrations

  2021influential citation
• Guidance document on the characterisation, validation and reporting of Physiologically Based Kinetic (PBK) models for regulatory purposes

  2021cites this paper
• Quantitation of Plasma Membrane Drug Transporters in Kidney Tissue and Cell Lines Using a Novel Proteomic Approach Enabled a Prospective Prediction of Metformin Disposition

  2021cites this paper
• Comparison between lab variability and in silico prediction errors for the unbound fraction of drugs in human plasma

  2021cites this paper
• Evaluation of drug‐drug interaction potential between omecamtiv mecarbil and rosuvastatin, a BCRP substrate, with a clinical study in healthy subjects and using a physiologically‐based pharmacokinetic model

  2021cites this paper
• Recent advances in drug transporter sciences: highlights from the year 2020

  2021cites this paper
• Cynomolgus Monkey as an Emerging Animal Model to Study Drug Transporters: In Vitro, In Vivo, In Vitro-to-In Vivo Translation

  2021influential citation
• A Mechanistic Site-Of-Action Model: A Tool for Informing Right Target, Right Compound, And Right Dose for Therapeutic Antagonistic Antibody Programs

  2021cites this paper
• Recent developments in in vitro and in vivo models for improved translation of preclinical pharmacokinetics and pharmacodynamics data

  2021cites this paper
• In/In Vivo Correlation for Transporters

  2020cites this paper
• Novel testing strategy for prediction of rat biliary excretion of intravenously administered estradiol-17β glucuronide

  2020cites this paper
• Effect of Human Plasma on Hepatic Uptake of Organic Anion–Transporting Polypeptide 1B Substrates: Studies Using Transfected Cells and Primary Human Hepatocytes

  2020influential citation
• In vitro-in vivo extrapolation of human hepatic and renal clearance

  2020cites this paper
• Prediction of Transporter-Mediated Rosuvastatin Hepatic Uptake Clearance and Drug Interaction in Humans Using Proteomics-Informed REF Approach

  2020cites this paper
• Quantitative Proteomics and Mechanistic Modeling of Transporter‐Mediated Disposition in Nonalcoholic Fatty Liver Disease

  2020cites this paper
• Evaluation of hepatic uptake of OATP1B substrates by short term-cultured plated human hepatocytes: Comparison with isolated suspended hepatocytes.

  2020cites this paper
• In Vitro Hepatic Uptake in Human and Monkey Hepatocytes in the Presence and Absence of Serum Protein and Its In Vitro to In Vivo Extrapolation

  2020cites this paper
• Albumin-Mediated Uptake Improves Human Clearance Prediction for Hepatic Uptake Transporter Substrates Aiding a Mechanistic In Vitro-In Vivo Extrapolation (IVIVE) Strategy in Discovery Research

  2020cites this paper
• Successful Prediction of Positron Emission Tomography–Imaged Metformin Hepatic Uptake Clearance in Humans Using the Quantitative Proteomics–Informed Relative Expression Factor Approach

  2020cites this paper
• Potential role of drug metabolizing enzymes in chemotherapy-induced gastrointestinal toxicity and hepatotoxicity

  2020cites this paper
• Predictability of human pharmacokinetics of drugs that undergo hepatic organic anion transporting polypeptide (OATP)-mediated transport using single-species allometric scaling in chimeric mice with humanized liver: integration with hepatic drug metabolism

  2020cites this paper
• Comparison of In Vitro to In Vivo Extrapolation Approaches for Predicting Transporter-Mediated Hepatic Uptake Clearance Using Suspended Rat Hepatocytes

  2020cites this paper
• Proteomics‐Informed Prediction of Rosuvastatin Plasma Profiles in Patients With a Wide Range of Body Weight

  2020cites this paper
• Successful prediction of PET-imaged metformin hepatic uptake clearance in humans using the quantitative proteomics-informed relative expression factor approach

  2020influential citation
• Predicting the Human Hepatic Clearance of Acidic and Zwitterionic Drugs.

  2020cites this paper
• Examination of Physiologically‐Based Pharmacokinetic Models of Rosuvastatin

  2020influential citation
• Use of imaging to assess the activity of hepatic transporters

  2020cites this paper
• Impact of Plasma Protein Binding in Drug Clearance Prediction: A Database Analysis of Published Studies and Implications for In Vitro-In Vivo Extrapolation

  2020cites this paper
• Prediction of Cyclosporin-Mediated Drug Interaction Using Physiologically Based Pharmacokinetic Model Characterizing Interplay of Drug Transporters and Enzymes

  2020cites this paper
• Predicting human tissue exposures to xenobiotics using a bottom-up physiologically-based biokinetic model.

  2020influential citation
• Transporter–enzyme interplay and the hepatic drug clearance: what have we learned so far?

  2020cites this paper
• Prediction of Transporter-Mediated Drug-Drug Interactions and Phenotyping of Hepatobiliary Transporters Involved in the Clearance of E7766, a Novel Macrocycle-Bridged Dinucleotide

  2020cites this paper
• A mechanistic modelling approach for the determination of the mechanisms of inhibition by cyclosporine on the uptake and metabolism of atorvastatin in rat hepatocytes using a high throughput uptake method

  2019cites this paper
• Quantitative translation of microfluidic transporter in vitro data to in vivo reveals impaired albumin-facilitated indoxyl sulfate secretion in chronic kidney disease.

  2019cites this paper
• Current Research Method in Transporter Study.

  2019cites this paper
• Utility of Chimeric Mice with Humanized Liver for Predicting Human Pharmacokinetics in Drug Discovery: Comparison with in Vitro-in Vivo Extrapolation and Allometric Scaling.

  2019cites this paper
• PBPK models for evaluating membrane transporter mediated DDIs: Current capabilities, case studies, future opportunities and recommendations.

  2019cites this paper
• Theoretical Considerations for Direct Translation of Unbound Liver-to-Plasma Partition Coefficient from In Vitro to In Vivo

  2019cites this paper
• The Presence of a Transporter-Induced Protein Binding Shift: A New Explanation for Protein-Facilitated Uptake and Improvement for In Vitro-In Vivo Extrapolation

  2019cites this paper
• Positron Emission Tomography Imaging of [11C]Rosuvastatin Hepatic Concentrations and Hepatobiliary Transport in Humans in the Absence and Presence of Cyclosporin A

  2019cites this paper
• Improvements for the in Vitro to in Vivo Extrapolation of Hepatic Clearance

  2019cites this paper
• A Novel Unified Approach to Predict Human Hepatic Clearance for Both Enzyme- and Transporter-Mediated Mechanisms Using Suspended Human Hepatocytes

  2019cites this paper
• Quantitative Contribution of Six Major Transporters to the Hepatic Uptake of Drugs: “SLC-Phenotyping” Using Primary Human Hepatocytes

  2019cites this paper
• The Regional-Specific Relative and Absolute Expression of Gut Transporters in Adult Caucasians: A Meta-Analysis

  2019cites this paper
• Recent advances in preclinical in vitro approaches towards quantitative prediction of hepatic clearance and drug-drug interactions involving organic anion transporting polypeptide (OATP) 1B transporters.

  2019cites this paper
• Structure-Activity Relationships of Efflux Transporter Inhibitors

  2019cites this paper
• Quantitative Prediction of Interactions Mediated by Transporters and Cytochromes: Application to Organic Anion Transporting Polypeptides, Breast Cancer Resistance Protein and Cytochrome 2C8

  2019cites this paper
• Changes in Organic Anion Transporting Polypeptide Uptake in HEK293 Overexpressing Cells in the Presence and Absence of Human Plasma

  2019cites this paper
• In Vitro/In Vivo Correlation for Transporters

  2019cites this paper
• A Comparison of Total and Plasma Membrane Abundance of Transporters in Suspended, Plated, Sandwich-Cultured Human Hepatocytes Versus Human Liver Tissue Using Quantitative Targeted Proteomics and Cell Surface Biotinylation

  2019cites this paper
• Bottom-up physiologically-based biokinetic modelling as an alternative to animal testing.

  2019cites this paper
• Successful Prediction of In Vivo Hepatobiliary Clearances and Hepatic Concentrations of Rosuvastatin Using Sandwich-Cultured Rat Hepatocytes, Transporter-Expressing Cell Lines, and Quantitative Proteomics

  2018cites this paper
• Noninvasive Preclinical and Clinical Imaging of Liver Transporter Function Relevant to Drug-Induced Liver Injury

  2018cites this paper
• Drug Transporters in Xenobiotic Disposition and Pharmacokinetic Prediction

  2018cites this paper
• Prediction of the Pharmacokinetics of Pravastatin as an OATP Substrate Using Plateable Human Hepatocytes With Human Plasma Data and PBPK Modeling

  2018influential citation
• Prediction and Quantification of Hepatic Transporter-Mediated Uptake of Pitavastatin Utilizing a Combination of the Relative Activity Factor Approach and Mechanistic Modeling

  2018cites this paper
• Navigating Transporter Sciences in Pharmacokinetics Characterization Using the Extended Clearance Classification System

  2018cites this paper
• Hepatic Organic Anion Transporting Polypeptide–Mediated Clearance in the Beagle Dog: Assessing In Vitro–In Vivo Relationships and Applying Cross-Species Empirical Scaling Factors to Improve Prediction of Human Clearance

  2018cites this paper