In vitroandin vivoapproaches to characterize transporter-mediated disposition in drug discovery

Quantitative assessment of the contribution of sodium-dependent taurocholate co-transporting polypeptide (NTCP) to the hepatic uptake of rosuvastatin, pitavastatin and fluvastatin

(2013) Yi-an Bi et al.   BIOPHARMACEUTICS & DRUG DISPOSITION

Pharmacokinetics of a Three-Way Drug Interaction Between Danoprevir, Ritonavir and the Organic Anion Transporting Polypeptide (OATP) Inhibitor Ciclosporin

(2013) Barbara J. Brennan et al.   CLINICAL PHARMACOKINETICS

In Vitro Methods to Support Transporter Evaluation in Drug Discovery and Development

(2013) K L R Brouwer et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Why Clinical Modulation of Efflux Transport at the Human Blood–Brain Barrier Is Unlikely: The ITC Evidence-Based Position

(2013) J C Kalvass et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Transporter Studies in Drug Development: Experience to Date and Follow-Up on Decision Trees From the International Transporter Consortium

(2013) D Tweedie et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Medicinal Chemistry Design Principles for Liver Targeting Through OATP Transporters

(2013) Meihua Tu et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Primary hepatocyte cultures as prominentin vitrotools to study hepatic drug transporters

(2013) Eva Ramboer et al.   DRUG METABOLISM REVIEWS

Effect of a single-dose rifampin on the pharmacokinetics of pitavastatin in healthy volunteers

(2013) Yao Chen et al.   EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY

PBPK models for the prediction of in vivo performance of oral dosage forms

(2013) Edmund S. Kostewicz et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Model-based approaches to predict drug–drug interactions associated with hepatic uptake transporters: preclinical, clinical and beyond

(2013) Hugh A Barton et al.   Expert Opinion on Drug Metabolism & Toxicology

LC–MS/MS-based quantification of clinically relevant intestinal uptake and efflux transporter proteins

(2013) C. Gröer et al.   JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS

Quantitative Prediction of Renal Transporter-Mediated Clinical Drug–Drug Interactions

(2013) Bo Feng et al.   MOLECULAR PHARMACEUTICS

Integration of in Silico and in Vitro Tools for Scaffold Optimization during Drug Discovery: Predicting P-Glycoprotein Efflux

(2013) Prashant V. Desai et al.   MOLECULAR PHARMACEUTICS

Mechanistic Modeling to Predict the Transporter- and Enzyme-Mediated Drug-Drug Interactions of Repaglinide

(2013) Manthena V. S. Varma et al.   PHARMACEUTICAL RESEARCH

A gene–gene interaction between polymorphisms in the OCT2 and MATE1 genes influences the renal clearance of metformin

(2013) Mette M.H. Christensen et al.   Pharmacogenetics and Genomics

Transporter-Mediated Drug–Drug Interactions Involving OATP Substrates: Predictions Based on In Vitro Inhibition Studies

(2012) K Yoshida et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Species differences in drug transporters and implications for translating preclinical findings to humans

(2012) Xiaoyan Chu et al.   Expert Opinion on Drug Metabolism & Toxicology

Classification of Inhibitors of Hepatic Organic Anion Transporting Polypeptides (OATPs): Influence of Protein Expression on Drug–Drug Interactions

(2012) Maria Karlgren et al.   JOURNAL OF MEDICINAL CHEMISTRY

Characterization of Organic Anion Transporting Polypeptide (OATP) Expression and Its Functional Contribution to the Uptake of Substrates in Human Hepatocytes

(2012) Emi Kimoto et al.   MOLECULAR PHARMACEUTICS

pH-Dependent Solubility and Permeability Criteria for Provisional Biopharmaceutics Classification (BCS and BDDCS) in Early Drug Discovery

(2012) Manthena V. Varma et al.   MOLECULAR PHARMACEUTICS

Physiologically Based Modeling of Pravastatin Transporter-Mediated Hepatobiliary Disposition and Drug-Drug Interactions

(2012) Manthena V. S. Varma et al.   PHARMACEUTICAL RESEARCH

Cyclosporine Inhibition of Hepatic and Intestinal CYP3A4, Uptake and Efflux Transporters: Application of PBPK Modeling in the Assessment of Drug-Drug Interaction Potential

(2012) Michael Gertz et al.   PHARMACEUTICAL RESEARCH

Evaluation of transporter-mediated hepatic uptake in a non-radioactive high-throughput assay: a study of kinetics, species difference and plasma protein effect

(2012) Ling Li et al.   XENOBIOTICA

Identification of the Rate-Determining Process in the Hepatic Clearance of Atorvastatin in a Clinical Cassette Microdosing Study

(2011) K Maeda et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Targeting Intestinal Transporters for Optimizing Oral Drug Absorption

(2011) Manthena V. Varma et al.   CURRENT DRUG METABOLISM

Advances in the Molecular Detection of ABC Transporters Involved in Multidrug Resistance in Cancer

(2011) Jean-Pierre Gillet et al.   CURRENT PHARMACEUTICAL BIOTECHNOLOGY

Prediction of Human Renal Clearance from Preclinical Species for a Diverse Set of Drugs That Exhibit Both Active Secretion and Net Reabsorption

(2011) S. W. Paine et al.   DRUG METABOLISM AND DISPOSITION

Kinetic Characterization of Rat Hepatic Uptake of 16 Actively Transported Drugs

(2011) Y. Yabe et al.   DRUG METABOLISM AND DISPOSITION

Prediction of the Overall Renal Tubular Secretion and Hepatic Clearance of Anionic Drugs and a Renal Drug-Drug Interaction Involving Organic Anion Transporter 3 in Humans by In Vitro Uptake Experiments

(2011) T. Watanabe et al.   DRUG METABOLISM AND DISPOSITION

Pharmacokinetic drug interaction between gemfibrozil and sitagliptin in healthy Indian male volunteers

(2011) Arun K. P. et al.   EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY

Development of a Liver-Targeted Stearoyl-CoA Desaturase (SCD) Inhibitor (MK-8245) to Establish a Therapeutic Window for the Treatment of Diabetes and Dyslipidemia

(2011) Renata M. Oballa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of (S)-6-(3-Cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic Acid as a Hepatoselective Glucokinase Activator Clinical Candidate for Treating Type 2 Diabetes Mellitus

(2011) Jeffrey A. Pfefferkorn et al.   JOURNAL OF MEDICINAL CHEMISTRY

Quantitative targeted absolute proteomics of human blood-brain barrier transporters and receptors

(2011) Yasuo Uchida et al.   JOURNAL OF NEUROCHEMISTRY

Quantitative Membrane Protein Expression at the Blood–Brain Barrier of Adult and Younger Cynomolgus Monkeys

(2011) Katsuaki Ito et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Development of a new permeability assay using low‐efflux MDCKII cells

(2011) Li Di et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Sodium fluorescein is a probe substrate for hepatic drug transport mediated by OATP1B1 and OATP1B3

(2011) Tom De Bruyn et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Quantitative Evaluation of the Impact of Active Efflux by P-Glycoprotein and Breast Cancer Resistance Protein at the Blood-Brain Barrier on the Predictability of the Unbound Concentrations of Drugs in the Brain Using Cerebrospinal Fluid Concentration as a Surrogate

(2011) H. Kodaira et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Transcriptomic and Quantitative Proteomic Analysis of Transporters and Drug Metabolizing Enzymes in Freshly Isolated Human Brain Microvessels

(2011) Ramzi Shawahna et al.   MOLECULAR PHARMACEUTICS

In Vitro and In Silico Strategies to Identify OATP1B1 Inhibitors and Predict Clinical Drug–Drug Interactions

(2011) Maria Karlgren et al.   PHARMACEUTICAL RESEARCH

Characterization of Organic Anion-Transporting Polypeptide (Oatp) 1a1 and 1a4 Null Mice Reveals Altered Transport Function and Urinary Metabolomic Profiles

(2011) Lei Gong et al.   TOXICOLOGICAL SCIENCES

Full efficacy with no CNS side-effects: unachievable panacea or reality? DMPK considerations in design of drugs with limited brain penetration

(2011) Susan Cole et al.   XENOBIOTICA

Fluorescence-based assays for the assessment of drug interaction with the human transporters OATP1B1 and OATP1B3

(2010) Dallas Bednarczyk   ANALYTICAL BIOCHEMISTRY

Mutual pharmacokinetic interactions between bosentan and lopinavir/ritonavir in healthy participants

(2010) Jasper Dingemanse et al.   ANTIVIRAL THERAPY

Predicting Drug Disposition via Application of a Biopharmaceutics Drug Disposition Classification System

(2010) Leslie Z. Benet   BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY

Characterization of Digoxin Uptake in Sandwich-Cultured Human Hepatocytes

(2010) E. Kimoto et al.   DRUG METABOLISM AND DISPOSITION

Renal clearance in drug discovery and development: molecular descriptors, drug transporters and disease state

(2010) Bo Feng et al.   Expert Opinion on Drug Metabolism & Toxicology

Organic anion transporting polypeptide 1a/1b–knockout mice provide insights into hepatic handling of bilirubin, bile acids, and drugs

(2010) Evita van de Steeg et al.   JOURNAL OF CLINICAL INVESTIGATION

Several Conserved Positively Charged Amino Acids in OATP1B1 are Involved in Binding or Translocation of Different Substrates

(2010) Yi M. Weaver et al.   JOURNAL OF MEMBRANE BIOLOGY

A Phase I Study of Vandetanib in Combination with Vinorelbine/Cisplatin or Gemcitabine/Cisplatin as First-Line Treatment for Advanced Non-small Cell Lung Cancer

(2010) Fiona H. Blackhall et al.   Journal of Thoracic Oncology

Improved Extrapolation of Hepatobiliary Clearance fromin VitroSandwich Cultured Rat Hepatocytes through Absolute Quantification of Hepatobiliary Transporters

(2010) Na Li et al.   MOLECULAR PHARMACEUTICS

Membrane transporters in drug development

(2010)   NATURE REVIEWS DRUG DISCOVERY

OCT2 polymorphisms and in-vivo renal functional consequence: studies with metformin and cimetidine

(2010) Zhi-Jun Wang et al.   Pharmacogenetics and Genomics

The effects of the SLCO2B1 c.1457C>T polymorphism and apple juice on the pharmacokinetics of fexofenadine and midazolam in humans

(2010) Junko Imanaga et al.   Pharmacogenetics and Genomics

Effect of P-glycoprotein-mediated efflux on cerebrospinal fluid concentrations in rhesus monkeys

(2009) Cuyue Tang et al.   BIOCHEMICAL PHARMACOLOGY

Role of basolateral efflux transporter MRP4 in the intestinal absorption of the antiviral drug adefovir dipivoxil

(2009) Xin Ming et al.   BIOCHEMICAL PHARMACOLOGY

Competitive inhibition of renal tubular secretion of ciprofloxacin and metabolite by probenecid

(2009) Cornelia B. Landersdorfer et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Impact of OATP transporters on pharmacokinetics

(2009) A Kalliokoski et al.   BRITISH JOURNAL OF PHARMACOLOGY

Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism

(2009) Yi-Jing He et al.   CLINICA CHIMICA ACTA

ABCG2 Polymorphism Markedly Affects the Pharmacokinetics of Atorvastatin and Rosuvastatin

(2009) J E Keskitalo et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Drug Transport Across the Blood-Brain Barrier and the Impact of Breast Cancer Resistance Protein (ABCG2)

(2009) Joseph Nicolazzo et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Silencing the Breast Cancer Resistance Protein Expression and Function in Caco-2 Cells Using Lentiviral Vector-Based Short Hairpin RNA

(2009) W. Zhang et al.   DRUG METABOLISM AND DISPOSITION

The Effect of Breast Cancer Resistance Protein and P-Glycoprotein on the Brain Penetration of Flavopiridol, Imatinib Mesylate (Gleevec), Prazosin, and 2-Methoxy-3-(4-(2-(5-methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)propanoic Acid (PF-407288) in Mice

(2009) L. Zhou et al.   DRUG METABOLISM AND DISPOSITION

Breast Cancer Resistance Protein Interacts with Various Compounds in Vitro, but Plays a Minor Role in Substrate Efflux at the Blood-Brain Barrier

(2009) R. Zhao et al.   DRUG METABOLISM AND DISPOSITION

Prediction of the Hepatic and Renal Clearance of Transporter Substrates in Rats Using in Vitro Uptake Experiments

(2009) T. Watanabe et al.   DRUG METABOLISM AND DISPOSITION

Effects of Atazanavir/Ritonavir or Fosamprenavir/Ritonavir on the Pharmacokinetics of Rosuvastatin

(2009) Anthony J Busti et al.   JOURNAL OF CARDIOVASCULAR PHARMACOLOGY

Prediction of pharmacokinetic profile of valsartan in human based on in vitro uptake transport data

(2009) Agnès Poirier et al.   JOURNAL OF PHARMACOKINETICS AND PHARMACODYNAMICS

Effect of genetic variation in the organic cation transporter 2 on the renal elimination of metformin

(2009) Ying Chen et al.   Pharmacogenetics and Genomics

Comparative gene expression profiles of ABC transporters in brain microvessel endothelial cells and brain in five species including human

(2009) Mark S. Warren et al.   PHARMACOLOGICAL RESEARCH

Effects of Gemfibrozil and Atorvastatin on the Pharmacokinetics of Repaglinide in Relation to SLCO1B1 Polymorphism

(2008) A Kalliokoski et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Elucidating Rifampin's Inducing and Inhibiting Effects on Glyburide Pharmacokinetics and Blood Glucose in Healthy Volunteers: Unmasking the Differential Effects of Enzyme Induction and Transporter Inhibition for a Drug and Its Primary Metabolite

(2008) HX Zheng et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Effect of an Antiretroviral Regimen Containing Ritonavir Boosted Lopinavir on Intestinal and Hepatic CYP3A, CYP2D6 and P-glycoprotein in HIV-infected Patients

(2008) C Wyen et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Methotrexate Pharmacokinetics in Transgenic Mice with Liver-Specific Expression of Human Organic Anion-Transporting Polypeptide 1B1 (SLCO1B1)

(2008) E. van de Steeg et al.   DRUG METABOLISM AND DISPOSITION

An Unexpected Synergist Role of P-Glycoprotein and Breast Cancer Resistance Protein on the Central Nervous System Penetration of the Tyrosine Kinase Inhibitor Lapatinib (N- -6-[5-( methyl)-2-furyl]-4-quinazolinamine; GW572016)

(2008) J. W. Polli et al.   DRUG METABOLISM AND DISPOSITION

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

(2008) A. Poirier et al.   DRUG METABOLISM AND DISPOSITION

Involvement of Multiple Transporters in the Hepatobiliary Transport of Rosuvastatin

(2008) S. Kitamura et al.   DRUG METABOLISM AND DISPOSITION

Species Differences in Blood-Brain Barrier Transport of Three Positron Emission Tomography Radioligands with Emphasis on P-Glycoprotein Transport

(2008) S. Syvanen et al.   DRUG METABOLISM AND DISPOSITION

Identification of interspecies difference in efflux transporters of hepatocytes from dog, rat, monkey and human

(2008) Meng Li et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

The Caco-2 cell monolayer: usefulness and limitations

(2008) Huadong Sun et al.   Expert Opinion on Drug Metabolism & Toxicology

Probenecid, but Not Cystic Fibrosis, Alters the Total and Renal Clearance of Fexofenadine

(2008) Shanshan Liu et al.   JOURNAL OF CLINICAL PHARMACOLOGY

The human brain endothelial cell line hCMEC/D3 as a human blood-brain barrier model for drug transport studies

(2008) Birk Poller et al.   JOURNAL OF NEUROCHEMISTRY

Methodology for development of a physiological model incorporating CYP3A and P-glycoprotein for the prediction of intestinal drug absorption

(2008) Raj Badhan et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

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

(2008) T. Watanabe et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

SLCO1B1Variants and Statin-Induced Myopathy — A Genomewide Study

(2008)   NEW ENGLAND JOURNAL OF MEDICINE

Cell models for studying renal physiology

(2008) M. Bens et al.   PFLUGERS ARCHIV-EUROPEAN JOURNAL OF PHYSIOLOGY

Characterization of Organic Anion Transporting Polypeptide 1b2-null Mice: Essential Role in Hepatic Uptake/Toxicity of Phalloidin and Microcystin-LR

(2008) Hong Lu et al.   TOXICOLOGICAL SCIENCES

Characterisation of human tubular cell monolayers as a model of proximal tubular xenobiotic handling

(2008) Colin D.A. Brown et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

A portal vein cannulation technique for drug discovery in mice

(2007) Xiaolan Shen et al.   LAB ANIMAL