Symposium Article: Molecular and Physical Mechanisms of First-Pass Extraction

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Human P-glycoprotein transports cyclosporin A and FK506.

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Role of intestinal P-glycoprotein (mdr1) in interpatient variation in the oral bioavailability of cyclosporine*

Lown, K. S., Mayo, R. R., Leichtman, A. B., Hsiao, H.-L., Turgeon, D. K., Schmiedlin‐Ren, P., Brown, M. B., Guo, W.-S., Rossi, S. J., Benet, L. Z., et al. (1997) · Clinical Pharmacology & Therapeutics · doi:10.1016/s0009-9236(97)90027-8 · Cited by 679 · see citing works

Human P-glycoprotein transports cortisol, aldosterone, and dexamethasone, but not progesterone.

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Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression.

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Oral first-pass elimination of midazolam involves both gastrointestinal and hepatic CYP3A-mediated metabolism*

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Identification of rifampin-inducible P450IIIA4 (CYP3A4) in human small bowel enterocytes.

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Identification of glucocorticoid-inducible cytochromes P-450 in the intestinal mucosa of rats and man.

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Prediction of in vivo drug metabolism in the human liver from in vitro metabolism data

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First-pass metabolism of cyclosporin by the gut

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Noninvasive tests of CYP3A enzymes

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Midazolam A Review of its Pharmacological Properties and Therapeutic Use

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

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Mechanisms of enhanced oral availability of CYP3A4 substrates by grapefruit constituents: Decreased enterocyte CYP3A4 concentration and mechanism-based inactivation by furanocoumarins

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Bioavailability of cyclosporine with concomitant rifampin administration is markedly less than predicted by hepatic enzyme induction

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First-pass metabolism of midazolam by the human intestine*

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Efficient inhibition of P-glycoprotein-mediated multidrug resistance with a monoclonal antibody.

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Interpatient heterogeneity in expression of CYP3A4 and CYP3A5 in small bowel: Lack of prediction by the erythromycin breath test

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The effects of ketoconazole on the intestinal metabolism and bioavailability of cyclosporine*

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Oxidation of dihydropyridine calcium channel blockers and analogs by human liver cytochrome P-450 IIIA4

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Possible Involvement of Multiple P-Glycoprotein-Mediated Efflux Systems in the Transport of Verapamil and Other Organic Cations Across Rat Intestine

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The function of Gp170, the multidrug-resistance gene product, in the brush border of rat intestinal mucosa

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The effect of water-soluble vitamin E on cyclosporine pharmacokinetics in healthy volunteers*

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Excretion and metabolism of 14C-midazolam in humans following oral dosing.

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Felodipine kinetics in healthy men

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Interpatient heterogeneity in expression of CYP3A4 and CYP3A5 in small bowel. Lack of prediction by the erythromycin breath test.

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P‐glycoprotein‐mediated transcellular transport of MDR‐reversing agents

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Ketoconazole Effectively Reverses Multidrug Resistance in Highly Resistant KB Cells

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Pharmacokinetics of felodipine in patients with liver disease

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From amplification to function: the case of the MDR1 gene

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Contribution of the intestine to the first-pass metabolism of felodipine in the rat.

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Enterohepatic Circulation

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Inhibition and induction of human cytochrome P450 enzymes: current status

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Physicochemical Space for Optimum Oral Bioavailability: Contribution of Human Intestinal Absorption and First-Pass Elimination

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Gut reactions: Breaking down xenobiotic–microbiome interactions

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Prediction of Human Intestinal First-Pass Metabolism of 25 CYP3A Substrates from In Vitro Clearance and Permeability Data

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Factors Influencing the Magnitude and Clinical Significance of Drug Interactions Between Azole Antifungals and Select Immunosuppressants

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The Influence of Age and Sex on the Clearance of Cytochrome P450 3A Substrates

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Unmasking the Dynamic Interplay between Intestinal P-Glycoprotein and CYP3A4

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P-Glycoprotein Increases from Proximal to Distal Regions of Human Small Intestine

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Knockout of cytochrome P450 3A yields new mouse models for understanding xenobiotic metabolism

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Dietary Effects on Drug Metabolism and Transport

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DIFFERENTIAL INTERACTION OF 3-HYDROXY-3-METHYLGLUTARYL-COA REDUCTASE INHIBITORS WITH ABCB1, ABCC2, AND OATP1B1

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Interactions between CYP3A4 and Dietary Polyphenols

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PREDICTION OF TIME-DEPENDENT CYP3A4 DRUG-DRUG INTERACTIONS: IMPACT OF ENZYME DEGRADATION, PARALLEL ELIMINATION PATHWAYS, AND INTESTINAL INHIBITION

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Intestinal and Hepatic Metabolic Activity of Five Cytochrome P450 Enzymes: Impact on Prediction of First-Pass Metabolism

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Down-Regulation of Intestinal Drug Transporters in Chronic Renal Failure in Rats

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Is the clinical relevance of drug-food and drug-herb interactions limited to grapefruit juice and Saint-John’s Wort?

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Potential role of intestinal first-pass metabolism in the prediction of drug–drug interactions

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Hepatic drug metabolism and transport in patients with kidney disease

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Contribution of Intestinal Cytochrome P450-Mediated Metabolism to Drug-Drug Inhibition and Induction Interactions

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Potentially Significant Drug Interactions of Class III Antiarrhythmic Drugs

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Enaminones: Exploring Additional Therapeutic Activities

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Cytochrome P4503APolymorphisms and Immunosuppressive Drugs: An Update

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A New Physiologically Based, Segregated-Flow Model to Explain Route-Dependent Intestinal Metabolism

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Association of MDR1, CYP3A4*18B, and CYP3A5*3 polymorphisms with cyclosporine pharmacokinetics in Chinese renal transplant recipients

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In Vitro Flow Cytometry Method to Quantitatively Assess Inhibitors of P-Glycoprotein

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The Role of P-Glycoprotein and Organic Anion-Transporting Polypeptides in Drug Interactions

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Midazolam Exhibits Characteristics of a Highly Permeable P-Glycoprotein Substrate

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Drug interactions during therapy with three major groups of antimicrobial agents

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The Evolving Role of Drug Metabolism in Drug Discovery and Development

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In Vivo use of the P450 inactivator 1-aminobenzotriazole in the rat: Varied dosing route to elucidate gut and liver contributions to first-pass and systemic clearance

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Toxicological hazard induced by sucralose to environmentally relevant concentrations in common carp (Cyprinus carpio)

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Screening of Genetic Polymorphisms ofCYP3A4andCYP3A5Genes

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How important is intestinal cytochrome P450 3A metabolism?

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Route-Dependent Metabolism of Morphine in the Vascularly Perfused Rat Small Intestine Preparation

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Rhabdomyolysis and Acute Renal Failure in a Cardiac Transplant Recipient due to Multiple Drug Interactions

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Glucuronidation of the Dietary Fatty Acids, Phytanic Acid and Docosahexaenoic Acid, by Human UDP-Glucuronosyltransferases

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Biochemical and analytical development of the CIME cocktail for drug fate assessment in humans

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Development of Murine Cyp3a Knockout Chimeric Mice with Humanized Liver

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The Pharmacogenetics of Immunosuppression for Organ Transplantation

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Advancing understanding of human variability through toxicokinetic modeling, in vitro-in vivo extrapolation, and new approach methodologies

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Polymer-surfactant nanoparticles for improving oral bioavailability of doxorubicin

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Modulation of P450 CYP3A4-Dependent Metabolism by P-glycoprotein: Implications for P450 Phenotyping

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Pharmacokinetics and Disposition of Silodosin (KMD-3213)

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Presystemic elimination of budesonide in man when administered locally at different levels in the gut, with and without local inhibition by ketoconazole

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Measurement of hepatic and intestinal CYP3A4 and PGP activity by combined po + iv [14C]erythromycin breath and urine test

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Contribution of Rat Pulmonary Metabolism to the Elimination of Lidocaine, Midazolam, and Nifedipine

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Influence of ABCB1, CYP3A4*18B and CYP3A5*3 polymorphisms on cyclosporine A pharmacokinetics in bone marrow transplant recipients

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An update on the use of transdermal oxybutynin in the management of overactive bladder disorder

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Managing drug interactions in the patient with aspergillosis

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Interactions médicaments–aliments en médecine interne : quels messages pour le clinicien ?

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Pharmacokinetics of ML3403 ({4-[5-(4-Fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-(1-phenylethyl)-amine), a 4-Pyridinylimidazole-Type p38 Mitogen-Activated Protein Kinase Inhibitor

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Explorations into modeling human oral bioavailability

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In Vitro–In Vivo Inaccuracy: The CYP3A4 Anomaly

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Differentiation of Gut and Hepatic First-Pass Effect of Drugs: 1. Studies of Verapamil in Ported Dogs

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Remofovir Mesylate: A Prodrug of PMEA with Improved Liver-Targeting and Safety in Rats and Monkeys

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Sex-dependent expression of CYP2C11 in spleen, thymus and bone marrow regulated by growth hormone

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In Vitro Techniques to Study Drug–Drug Interactions of Drug Metabolism: Cytochrome P450

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Basolateral and canalicular transport of xenobiotics in the hepatocyte: A review

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AUTOINDUCTION OF MKC-963 [(R)-1-(1-CYCLOHEXYLETHYLAMINO)-4-PHENYLPHTHALAZINE] METABOLISM IN HEALTHY VOLUNTEERS AND ITS RETROSPECTIVE EVALUATION USING PRIMARY HUMAN HEPATOCYTES AND CDNA-EXPRESSED ENZYMES

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The Role of Sulfotransferases (SULTs) and UDP-Glucuronosyltransferases (UGTs) in Human Drug Clearance and Bioactivation

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Mechanisms of Drug Interactions I: Absorption, Metabolism, and Excretion

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Upholding or Breaking the Law of Superposition in Pharmacokinetics

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Genetic variance in ABCB1 and CYP3A5 does not contribute toward the development of chronic kidney disease after liver transplantation

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Treating mood disorders in patients with a history of intestinal surgery

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An Economic Model of 2-Hour Post-Dose Ciclosporin Monitoring in Renal Transplantation

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Determination of Appropriate Dosing of Influenza Drugs in Pediatric Patients

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Molecular cloning and expression analysis of cytochrome P450 3A gene in the turbot Scophthalmus maximus

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Intestinal CYP3A4 is not involved in the enantioselective disposition of lansoprazole

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Role of P-Glycoprotein and the Intestine in the Excretion of DPC 333 [(2R)-2-{(3R)-3-Amino-3-[4-(2-methylquinolin-4-ylmethoxy)phenyl]-2-oxopyrrolidin-1-yl}-N-hydroxy-4-methylpentanamide] in Rodents

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Drug Metabolism and Chronic Kidney Disease

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Mechanisms of Drug Interactions

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Presystemic Elimination of Trichloroethylene in Rats Following Environmentally Relevant Oral Exposures

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Antifungal therapeutic drug monitoring: When, how, and why

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Effect of Ketoconazole on Lobeglitazone Pharmacokinetics in Korean Volunteers

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Modeling and Simulation of Pharmacokinetic Aspects of Cytochrome P450-Based Metabolic Drug–Drug Interactions

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PEDIATRIC PHARMACOLOGY

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Semi-mechanistic population pharmacokinetic model incorporating glutathione S-transferase activity for personalized busulfan dosing in pediatric allogeneic hematopoietic cell transplantation

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SPURIOUS OBSERVATION OF SPLENIC CYP2B1 EXPRESSION

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Transfert des polluants organiques persistants (POP) du fourrage vers le lait chez le ruminant

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Biomechanics for Pathology and Treatment

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Drug Interactions in Solid Organ Transplant Recipients

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Antifungal Drug Interactions

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Influence of intestinal microbiota on the metabolism of main cardiotropic drugs

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Stereoselective Renal Elimination

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Human Oral Bioavailability Prediction of Four Kinds of Drugs

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Impact of intestinal metabolism on drug development

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Abstracts of Symposium Presentations (Monday)

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Abstracts of Symposium Presentations (Thursday)

(2001) · Drug Metabolism Reviews · doi:10.1081/dmr-100106329

Abstracts of Symposium Presentations (Tuesday)

(2001) · Drug Metabolism Reviews · doi:10.1081/dmr-100106289

Abstracts of Symposium Presentations (Wednesday)

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First-pass metabolism.

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