The Role of Transporters in the Pharmacokinetics of Orally Administered Drugs

Functional polymorphisms of the human multidrug-resistance gene: Multiple sequence variations and correlation of one allele with P-glycoprotein expression and activity in vivo

2000 • 2,358 citations

Predicting Drug Disposition via Application of BCS: Transport/Absorption/ Elimination Interplay and Development of a Biopharmaceutics Drug Disposition Classification System

2005 • 1,348 citations

The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin

1999 • 911 citations

Regulation of Multidrug Resistance-associated Protein 2 (ABCC2) by the Nuclear Receptors Pregnane X Receptor, Farnesoid X-activated Receptor, and Constitutive Androstane Receptor

2002 • 888 citations

Nuclear Receptor Response Elements Mediate Induction of Intestinal MDR1 by Rifampin

2001 • 843 citations

Molecular Properties of WHO Essential Drugs and Provisional Biopharmaceutical Classification

2003 • 839 citations

Waiver of In Vivo Bioavailability and Bioequivalence Studies for Immediate-Release Solid Oral Dosage Forms Based on a Biopharmaceutics Classification System

2001 • 786 citations

Human Bile Salt Export Pump Promoter Is Transactivated by the Farnesoid X Receptor/Bile Acid Receptor

2001 • 753 citations

Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver

2001 • 722 citations

Potent and specific inhibition of the breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C.

2002 • 682 citations

Nuclear Pregnane X Receptor and Constitutive Androstane Receptor Regulate Overlapping but Distinct Sets of Genes Involved in Xenobiotic Detoxification

2002 • 642 citations

Expression of Thirty-six Drug Transporter Genes in Human Intestine, Liver, Kidney, and Organotypic Cell Lines

2007 • 574 citations

A Provisional Biopharmaceutical Classification of the Top 200 Oral Drug Products in the United States, Great Britain, Spain, and Japan

2006 • 565 citations

Polymorphisms of OATP-C (SLC21A6) and OAT3 (SLC22A8) genes: Consequences for pravastatin pharmacokinetics

2003 • 514 citations

Effect of Genetic Variation in the Organic Cation Transporter 1, OCT1, on Metformin Pharmacokinetics

2007 • 461 citations

The Multidrug Resistance Protein 5 Functions as an ATP-dependent Export Pump for Cyclic Nucleotides

2000 • 438 citations

Different Effects of SLCO1B1 Polymorphism on the Pharmacokinetics of Atorvastatin and Rosuvastatin

2007 • 414 citations

Predicting drug disposition, absorption/elimination/transporter interplay and the role of food on drug absorption

2007 • 409 citations

Comparison of human duodenum and Caco-2 gene expression profiles for 12,000 gene sequences tags and correlation with permeability of 26 drugs.

2002 • 406 citations

Xenobiotic transporters of the human organic anion transporting polypeptides (OATP) family

2008 • 406 citations

Intestinal Drug Transporter Expression and the Impact of Grapefruit Juice in Humans

2007 • 400 citations

Structure, Function, Expression, Genomic Organization, and Single Nucleotide Polymorphisms of Human ABCB1 (MDR1), ABCC (MRP), and ABCG2 (BCRP) Efflux Transporters

2006 • 395 citations

P-glycoprotein: a defense mechanism limiting oral bioavailability and CNS accumulation of drugs

2000 • 382 citations

Why is it Challenging to Predict Intestinal Drug Absorption and Oral Bioavailability in Human Using Rat Model

2006 • 371 citations

Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver

2002 • 369 citations

Nuclear Receptors and the Regulation of Drug‐Metabolizing Enzymes and Drug Transporters: Implications for Interindividual Variability in Response to Drugs

2007 • 362 citations

Polymorphic organic anion transporting polypeptide 1B1 is a major determinant of repaglinide pharmacokinetics

2005 • 358 citations

Polymorphisms in Human Organic Anion-transporting Polypeptide 1A2 (OATP1A2)

2005 • 351 citations

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

2008 • 345 citations

Substrates and Inhibitors of Human Multidrug Resistance Associated Proteins and the Implications in Drug Development

2008 • 343 citations

Differentiation of absorption and first-pass gut and hepatic metabolism in humans: Studies with cyclosporine*

1995 • 342 citations

Human Organic Anion Transporting Polypeptide-C (SLC21A6) Is a Major Determinant of Rifampin-Mediated Pregnane X Receptor Activation

2003 • 325 citations

Effect of OATP1B Transporter Inhibition on the Pharmacokinetics of Atorvastatin in Healthy Volunteers

2006 • 315 citations

Novel membrane transporter OCTN1 mediates multispecific, bidirectional, and pH-dependent transport of organic cations.

1999 • 308 citations

Several major antiepileptic drugs are substrates for human P-glycoprotein

2008 • 296 citations

Evidence for inverse effects of OATP-C (SLC21A6) *5 and *1b haplotypes on pravastatin kinetics

2004 • 293 citations

Intestinal MDR transport proteins and P-450 enzymes as barriers to oral drug delivery

1999 • 292 citations

Unmasking the Dynamic Interplay between Intestinal P-Glycoprotein and CYP3A4

2002 • 286 citations

Naringin is a Major and Selective Clinical Inhibitor of Organic Anion-Transporting Polypeptide 1A2 (OATP1A2) in Grapefruit Juice

2007 • 281 citations

Induction of P-glycoprotein by rifampin increases intestinal secretion of talinolol in human beings: A new type of drug/drug interaction

2000 • 281 citations

Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3

2002 • 279 citations

Intestinal permeability and its relevance for absorption and elimination

2007 • 270 citations

Role of human MDR1 gene polymorphism in bioavailability and interaction of digoxin, a substrate of P‐glycoprotein

2002 • 268 citations

Coordinate regulation of xenobiotic and bile acid homeostasis by pregnane X receptor.

2001 • 255 citations

Pharmacokinetic Interactions of Drugs with St John’s Wort

2004 • 254 citations

Comparison of drug transporter gene expression and functionality in Caco-2 cells from 10 different laboratories

2008 • 253 citations

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

2007 • 248 citations

Role of BCRP 421C>A polymorphism on rosuvastatin pharmacokinetics in healthy Chinese males

2006 • 247 citations

MDR3 P-glycoprotein, a Phosphatidylcholine Translocase, Transports Several Cytotoxic Drugs and Directly Interacts with Drugs as Judged by Interference with Nucleotide Trapping

2000 • 246 citations

Diflomotecan pharmacokinetics in relation to ABCG2 421C>A genotype*1

2004 • 241 citations

Metformin Transport by a Newly Cloned Proton-Stimulated Organic Cation Transporter (Plasma Membrane Monoamine Transporter) Expressed in Human Intestine

2007 • 234 citations

Variability in Caco-2 and MDCK Cell-Based Intestinal Permeability Assays

2007 • 231 citations

Interactions between Hepatic Mrp4 and Sult2a as Revealed by the Constitutive Androstane Receptor and Mrp4 Knockout Mice

2004 • 229 citations

Antimalarial Artemisinin Drugs Induce Cytochrome P450 and MDR1 Expression by Activation of Xenosensors Pregnane X Receptor and Constitutive Androstane Receptor

2005 • 220 citations

Oatp2 Mediates Bidirectional Organic Solute Transport: A Role for Intracellular Glutathione

2000 • 219 citations

Mice lacking multidrug resistance protein 3 show altered morphine pharmacokinetics and morphine-6-glucuronide antinociception

2005 • 213 citations

Organic anion transporting polypeptide 2B1 is a high-affinity transporter for atorvastatin and is expressed in the human heart

2006 • 209 citations

Interaction of Organic Cations with a Newly Identified Plasma Membrane Monoamine Transporter

2005 • 187 citations

Identification of Thyroid Hormone Transporters in Humans: Different Molecules Are Involved in a Tissue-Specific Manner*,†

2001 • 183 citations

Organic Anion Transporting Polypeptide Mediates Organic Anion/HCO3− Exchange

1997 • 179 citations

Bile Salt Export Pump (BSEP/ABCB11) Can Transport a Nonbile Acid Substrate, Pravastatin

2005 • 174 citations

Peroxisome Proliferator-activated Receptor γ-regulated ABCG2 Expression Confers Cytoprotection to Human Dendritic Cells

2006 • 171 citations

Irinotecan-induced Diarrhea: Functional Significance of the Polymorphic ABCC2 Transporter Protein

2006 • 170 citations

Human organic anion transporting polypeptide 8 promoter is transactivated by the farnesoid X receptor/bile acid receptor

2002 • 167 citations

ATP-binding cassette, subfamily G (ABCG family)

2006 • 165 citations

Impact of Genetic Polymorphisms of Transporters on the Pharmacokinetic, Pharmacodynamic and Toxicological Properties of Anionic Drugs

2008 • 162 citations

SLCO1B1 (OATP1B1, an Uptake Transporter) and ABCG2 (BCRP, an Efflux Transporter) Variant Alleles and Pharmacokinetics of Pitavastatin in Healthy Volunteers

2007 • 158 citations

In Vivo Modulation of Intestinal CYP3A Metabolism by P-Glycoprotein: Studies Using the Rat Single-Pass Intestinal Perfusion Model

2003 • 157 citations

Segmental Dependent Transport of Low Permeability Compounds along the Small Intestine Due to P-Glycoprotein: The Role of Efflux Transport in the Oral Absorption of BCS Class III Drugs

2008 • 157 citations

Effect of ABCG2 genotype on the oral vioavailability of topotecan

2005 • 154 citations

Profiling SLCO and SLC22 genes in the NCI-60 cancer cell lines to identify drug uptake transporters

2008 • 153 citations

Characterization of two splice variants of human organic anion transporting polypeptide 3A1 isolated from human brain

2006 • 153 citations

Differential Modulation of the Human Liver Conjugate Transporters MRP2 and MRP3 by Bile Acids and Organic Anions

2003 • 152 citations

Influence of SLCO1B1, 1B3, 2B1 and ABCC2 genetic polymorphisms on mycophenolic acid pharmacokinetics in Japanese renal transplant recipients

2007 • 147 citations

Bile acid transporters in health and disease

2008 • 145 citations

Transport of antiviral 3′-deoxy-nucleoside drugs by recombinant human and rat equilibrative, nitrobenzylthioinosine (NBMPR)-insensitive (ENT2) nucleoside transporter proteins produced in Xenopus oocytes

2001 • 144 citations

ABCB1 Pharmacogenetics: Progress, Pitfalls, and Promise

2007 • 141 citations

Breast cancer resistance protein (ABCG2) and drug disposition: intestinal expression, polymorphisms and sulfasalazine as an in vivo probe

2008 • 137 citations

The Use of BDDCS in Classifying the Permeability of Marketed Drugs

2008 • 137 citations

Expression of the Steroid and Xenobiotic Receptor and Its Possible Target Gene, Organic Anion Transporting Polypeptide-A, in Human Breast Carcinoma

2006 • 134 citations

Effects of Drug Transporters on Volume of Distribution

2009 • 133 citations

Physiology, structure, and regulation of the cloned organic anion transporters

2008 • 131 citations

Differential Inhibition of Rat and Human Na⁺-Dependent Taurocholate Cotransporting Polypeptide (NTCP/SLC10A1)by Bosentan: A Mechanism for Species Differences in Hepatotoxicity

2007 • 129 citations

Induction of Intestinal P-glycoprotein by St John's Wort Reduces the Oral Bioavailability of Talinolol

2007 • 128 citations

Inhibition of the epidermal growth factor receptor increases expression of genes that stimulate inflammation, apoptosis, and cell attachment

2005 • 127 citations

The Human Na+-Taurocholate Cotransporting Polypeptide Gene Is Activated by Glucocorticoid Receptor and Peroxisome Proliferator-Activated Receptor-γ Coactivator-1α, and Suppressed by Bile Acids via a Small Heterodimer Partner-Dependent Mechanism

2005 • 127 citations

MRP class of human ATP binding cassette (ABC) transporters: historical background and new research directions

2008 • 123 citations

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 • 122 citations

The effect of SLCO1B1*15 on the disposition of pravastatin and pitavastatin is substrate dependent: the contribution of transporting activity changes by SLCO1B1*15

2008 • 121 citations

Breast Cancer Resistance Protein (Bcrp1/Abcg2) Limits Net Intestinal Uptake of Quercetin in Rats by Facilitating Apical Efflux of Glucuronides

2005 • 121 citations

Organic cation transporters

2008 • 121 citations

Applications of Physiologically Based Absorption Models in Drug Discovery and Development

2008 • 118 citations

Human organic anion transporter 1B1 and 1B3 function as bidirectional carriers and do not mediate GSH-bile acid cotransport

2007 • 116 citations

Pharmacogenetics of OATP ( SLC21 / SLCO ), OAT and OCT ( SLC22 ) and PEPT ( SLC15 ) Transporters in the Intestine, Liver and Kidney

2008 • 112 citations

A variant 2677A allele of the gene affects fexofenadine disposition

2004 • 112 citations

Challenges and opportunities with modelling and simulation in drug discovery and drug development

2007 • 111 citations

Role of MRP4 and MRP5 in biology and chemotherapy

2002 • 111 citations

Human Organic Anion-Transporting Polypeptide OATP-A (SLC21A3) Acts in Concert with P-Glycoprotein and Multidrug Resistance Protein 2 in the Vectorial Transport of Saquinavir in Hep G2 Cells

2003 • 109 citations

Kinetic Analyses for Species Differences in P-glycoprotein-Mediated Drug Transport

2006 • 107 citations

Distribution of monocarboxylate transporters MCT1-MCT8 in rat tissues and human skeletal muscle

2006 • 106 citations

The Role of Placental Breast Cancer Resistance Protein in the Efflux of Glyburide across the Human Placenta

2008 • 103 citations

FUNCTIONAL EXPRESSION OF SINUSOIDAL DRUG TRANSPORTERS IN PRIMARY HUMAN AND RAT HEPATOCYTES

2005 • 103 citations

Substrate Overlap between Mrp4 and Abcg2/Bcrp Affects Purine Analogue Drug Cytotoxicity and Tissue Distribution

2007 • 100 citations

Effect of SLCO1B1 genetic polymorphism on the pharmacokinetics of nateglinide

2006 • 99 citations

Monocarboxylate transporter 1 (MCT1) plays a direct role in short‐chain fatty acids absorption in caprine rumen

2006 • 98 citations

Absolute Difference of Hepatobiliary Transporter Multidrug Resistance-Associated Protein (MRP2/Mrp2) in Liver Tissues and Isolated Hepatocytes from Rat, Dog, Monkey, and Human

2008 • 96 citations

Organic anion transporting polypeptide 1B1 activity classified by SLCO1B1 genotype influences atrasentan pharmacokinetics

2006 • 96 citations

Drug Metabolizing Enzymes

2003 • 95 citations

The Operational Multiple Dosing Half-life: A Key to Defining Drug Accumulation in Patients and to Designing Extended Release Dosage Forms

2008 • 94 citations

Modulation by drugs of human hepatic sodium-dependent bile acid transporter (sodium taurocholate cotransporting polypeptide) activity.

1999 • 93 citations

Comparison of "type I" and "type II" organic cation transport by organic cation transporters and organic anion-transporting polypeptides.

2001 • 91 citations

Pharmacodynamics of Carbamazepine-mediated Induction of CYP3A4, CYP1A2, and Pgp as Assessed by Probe Substrates Midazolam, Caffeine, and Digoxin

2007 • 91 citations

Pharmacogenetics of SLCO1B1 gene and the impact of *1b and *15 haplotypes on irinotecan disposition in Asian cancer patients

2006 • 90 citations

Biopharmaceutics Classification of Selected β-Blockers: Solubility and Permeability Class Membership

2007 • 90 citations

Localization of organic anion transporting polypeptides in the rat and human ciliary body epithelium

2004 • 88 citations

Inhibition of multidrug transporters by verapamil or probenecid does not alter blood-brain barrier penetration of levetiracetam in rats

2004 • 88 citations

FXR-activating ligands inhibit rabbit ASBT expression via FXR-SHP-FTF cascade

2004 • 85 citations

Functional and Genetic Diversity in the Concentrative Nucleoside Transporter, CNT1, in Human Populations

2004 • 84 citations

Concentration-Dependent Effect of Naringin on Intestinal Absorption of β1-Adrenoceptor Antagonist Talinolol Mediated by P-Glycoprotein and Organic Anion Transporting Polypeptide (Oatp)

2008 • 83 citations

Involvement of MRP4 (ABCC4) in the Luminal Efflux of Ceftizoxime and Cefazolin in the Kidney

2007 • 83 citations

Gene Expression in the Human Intestine and Correlation with Oral Valacyclovir Pharmacokinetic Parameters

2003 • 82 citations

Establishment of a Set of Double Transfectants Coexpressing Organic Anion Transporting Polypeptide 1B3 and Hepatic Efflux Transporters for the Characterization of the Hepatobiliary Transport of Telmisartan Acylglucuronide

2008 • 80 citations

Distribution and function of the peptide transporter PEPT2 in normal and cystic fibrosis human lung

2002 • 79 citations

Permeability Dominates in Vivo Intestinal Absorption of P-gp Substrate with High Solubility and High Permeability

2005 • 77 citations

Application and limitation of inhibitors in drug–transporter interactions studies

2007 • 75 citations

Drug Transporters: Their Role and Importance in the Selection and Development of New Drugs

2002 • 74 citations

A LC–MS/MS method to quantify the novel cholesterol lowering drug ezetimibe in human serum, urine and feces in healthy subjects genotyped for SLCO1B1

2005 • 74 citations

The effect of ketoconazole on the in vivo intestinal permeability of fexofenadine using a regional perfusion technique

2003 • 74 citations

Characterization of Substrates and Inhibitors for the In Vitro Assessment of Bcrp Mediated Drug–Drug Interactions

2008 • 73 citations

Topotecan Is a Substrate for Multidrug Resistance Associated Protein 4

2005 • 72 citations

Involvement of influx and efflux transport systems in gastrointestinal absorption of celiprolol

2008 • 72 citations

Leflunomide and its metabolite A771726 are high affinity substrates of BCRP: implications for drug resistance

2008 • 70 citations

Interactions of Human- and Rat-Organic Anion Transporters With Pravastatin and Cimetidine

2004 • 68 citations

Involvement of Multidrug Resistance-Associated Protein 2 (Abcc2) in Molecular Weight-Dependent Biliary Excretion of β-Lactam Antibiotics

2008 • 68 citations

Effects of Grapefruit Juice on Intestinal P‐glycoprotein: Evaluation Using Digoxin in Humans

2003 • 65 citations

Hepatic drug transporters and nuclear receptors: Regulation by therapeutic agents

2008 • 60 citations

MDR1 genotype-related duodenal absorption rate of digoxin in healthy Japanese subjects.

2003 • 60 citations

A Novel Inhibitor of the Mammalian Peptide Transporter PEPT1

2001 • 55 citations

Expression and localization of organic cation/carnitine transporter OCTN2 in Caco-2 cells

2003 • 53 citations

Expression, Localisation and Activity of ATP Binding Cassette (ABC) Family of Drug Transporters in Human Amnion Membranes

2007 • 53 citations

Genetic analysis and functional characterization of polymorphisms in the human concentrative nucleoside transporter, CNT2

2005 • 51 citations

Nitric oxide reduces adenosine transporter ENT1 gene (SLC29A1) promoter activity in human fetal endothelium from gestational diabetes

2006 • 50 citations

4‐Aminomethylbenzoic acid is a non‐translocated competitive inhibitor of the epithelial peptide transporter PepT1

1998 • 50 citations

The Use of Drug Metabolism for Prediction of Intestinal Permeability

2009 • 49 citations

Altered Oral Bioavailability and Pharmacokinetics of P-Glycoprotein Substrates by Coadministration of Biochanin A

2006 • 47 citations

Cultured CD4T cells and primary human lymphocytes express hOATPs: intracellular accumulation of saquinavir and lopinavir

2008 • 44 citations

Impact of Basolateral Multidrug Resistance-Associated Protein (Mrp) 3 and Mrp4 on the Hepatobiliary Disposition of Fexofenadine in Perfused Mouse Livers

2008 • 43 citations

Orange juice increased the bioavailability of pravastatin, 3-hydroxy-3-methylglutaryl CoA reductase inhibitor, in rats and healthy human subjects

2006 • 41 citations

The MDCK cell line is made up of populations of cells with diverse resistive and transport properties

2000 • 41 citations

Minimal effect of MDR1 and CYP3A5 genetic polymorphisms on the pharmacokinetics of indinavir in HIV‐infected patients

2007 • 40 citations

Activation of CFTR by ASBT-mediated bile salt absorption

2005 • 37 citations

The Role of Permeability in Drug ADME/PK, Interactions and Toxicity—Presentation of a Permeability-Based Classification System (PCS) for Prediction of ADME/PK in Humans

2007 • 37 citations

Using novobiocin as a specific inhibitor of breast cancer resistant protein to assess the role of transporter in the absorption and disposition of topotecan

2007 • 36 citations

Differential kinetics of transport of 2',3'-dideoxyinosine and adenosine via concentrative Na+ nucleoside transporter CNT2 cloned from rat blood-brain barrier.

2001 • 35 citations

Multidrug resistance protein-6 (MRP6) in human dermal fibroblasts. Comparison between cells from normal subjects and from Pseudoxanthoma elasticum patients

2003 • 34 citations

Synthesis, Flow Cytometric Evaluation, and Identification of Highly Potent Dipyridamole Analogues as Equilibrative Nucleoside Transporter 1 Inhibitors

2007 • 33 citations

Pharmacogenetics of Intestinal Absorption

2008 • 32 citations

A Possible Role of Multidrug Resistance–Associated Protein 2 (Mrp2) in Hepatic Excretion of PCB126, an Environmental Contaminant: PBPK/PD Modeling

2008 • 26 citations

Glucuronidation Converting Methyl 1-(3,4-Dimethoxyphenyl)-3-(3-ethylvaleryl)-4-hydroxy-6,7,8-trimethoxy-2-naphthoate (S-8921) to a Potent Apical Sodium-Dependent Bile Acid Transporter Inhibitor, Resulting in a Hypocholesterolemic Action

2007 • 23 citations

Explorations into modeling human oral bioavailability

2008 • 19 citations

Hypoxanthine uptake and release by equilibrative nucleoside transporter 2 (ENT2) of rat microvascular endothelial cells

2007 • 18 citations

Endogenous expression of liver-specific drug transporters for organic anions in the rat hepatocytoma fusion cell line HPCT-1E3

2005 • 11 citations

Interaction of nucleoside‐derivatives with the human Na ⁺ /nucleoside cotransporters CNT1 and CNT3

2008 • 1 citations

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