Metformin and cimetidine: Physiologically based pharmacokinetic modelling to investigate transporter mediated drug-drug interactions.

[1]  H. Lindén,et al.  The European Federation for Pharmaceutical Sciences , 2003 .

[2]  Yuichi Sugiyama,et al.  A Species Difference in the Transport Activities of H2 Receptor Antagonists by Rat and Human Renal Organic Anion and Cation Transporters , 2005, Journal of Pharmacology and Experimental Therapeutics.

[3]  Malcolm Rowland,et al.  Mechanistic Approaches to Volume of Distribution Predictions: Understanding the Processes , 2007, Pharmaceutical Research.

[4]  Joanne Wang,et al.  Metformin Transport by a Newly Cloned Proton-Stimulated Organic Cation Transporter (Plasma Membrane Monoamine Transporter) Expressed in Human Intestine , 2007, Drug Metabolism and Disposition.

[5]  L. Benet,et al.  Food intake and dosage level, but not tablet vs solution dosage form, affect the absorption of metformin HC1 in man , 1996 .

[6]  Y. Moriyama,et al.  Role of glutamate residues in substrate recognition by human MATE1 polyspecific H+/organic cation exporter. , 2008, American journal of physiology. Cell physiology.

[7]  H. Koepsell,et al.  Polyspecific Organic Cation Transporters: Structure, Function, Physiological Roles, and Biopharmaceutical Implications , 2007, Pharmaceutical Research.

[8]  L. Benet,et al.  Food intake and dosage level, but not tablet vs solution dosage form, affect the absorption of metformin HCl in man. , 1996, British journal of clinical pharmacology.

[9]  M. Jamei,et al.  A Mechanistic Framework for In Vitro–In Vivo Extrapolation of Liver Membrane Transporters: Prediction of Drug–Drug Interaction Between Rosuvastatin and Cyclosporine , 2013, Clinical Pharmacokinetics.

[10]  J. Thiffault,et al.  Bioavailability of metformin in tablet form using a new high pressure liquid chromatography assay method , 1993, Biopharmaceutics & drug disposition.

[11]  H. Koepsell.  Substrate recognition and translocation by polyspecific organic cation transporters , 2011, Biological chemistry.

[12]  Ute Hofmann,et al.  Proton Pump Inhibitors Inhibit Metformin Uptake by Organic Cation Transporters (OCTs) , 2011, PloS one.

[13]  Conrad C. Huang,et al.  The human organic anion transporter 3 (OAT3; SLC22A8): genetic variation and functional genomics. , 2006, American journal of physiology. Renal physiology.

[14]  Y. Sogame,et al.  A comparison of uptake of metformin and phenformin mediated by hOCT1 in human hepatocytes , 2009, Biopharmaceutics & drug disposition.

[15]  P. Barts,et al.  Effects of membrane potential and surface potential on the kinetics of solute transport , 1985 .

[16]  G. Franceschini,et al.  Disposition of metformin (N,N‐dimethylbiguanide) in man , 1978, Clinical pharmacology and therapeutics.

[17]  B. Feng,et al.  Physiologically Based Modeling of Pravastatin Transporter-Mediated Hepatobiliary Disposition and Drug-Drug Interactions , 2012, Pharmaceutical Research.

[18]  A. Avdeef,et al.  pH-metric solubility. 3. Dissolution titration template method for solubility determination. , 2001, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[19]  Masoud Jamei,et al.  Application of permeability-limited physiologically-based pharmacokinetic models: part I-digoxin pharmacokinetics incorporating P-glycoprotein-mediated efflux. , 2013, Journal of pharmaceutical sciences.

[20]  L. Benet,et al.  Pharmacokinetics and Pharmacodynamics of Metformin in Healthy Subjects and Patients with Noninsulin‐Dependent Diabetes Mellitus , 1996, Journal of clinical pharmacology.

[21]  F. Russel,et al.  Semi-mechanistic physiologically-based pharmacokinetic modeling of clinical glibenclamide pharmacokinetics and drug-drug-interactions. , 2013, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[22]  Eun Sug Park,et al.  Verapamil decreases the glucose-lowering effect of metformin in healthy volunteers. , 2014, British journal of clinical pharmacology.

[23]  Paul D. Martin,et al.  Pharmacokinetic Evaluations of the Co-Administrations of Vandetanib and Metformin, Digoxin, Midazolam, Omeprazole or Ranitidine , 2014, Clinical Pharmacokinetics.

[24]  L. Benet,et al.  Kidney Function and Age Are Both Predictors of Pharmacokinetics of Metformin , 1995, Journal of clinical pharmacology.

[25]  A. Somogyi,et al.  Impaired cimetidine absorption due to antacids and metoclopramide , 2004, European Journal of Clinical Pharmacology.

[26]  I Meineke,et al.  The Effects of Genetic Polymorphisms in the Organic Cation Transporters OCT1, OCT2, and OCT3 on the Renal Clearance of Metformin , 2009, Clinical pharmacology and therapeutics.

[27]  Thomas K. H. Chang,et al.  The effect of cimetidine on dextromethorphan O-demethylase activity of human liver microsomes and recombinant CYP2D6. , 2004, Drug metabolism and disposition: the biological fate of chemicals.

[28]  HighWire Press,et al.  Drug metabolism and disposition : the biological fate of chemicals. , 1973 .

[29]  P. Neuvonen,et al.  Pharmacokinetics of metformin after intravenous and oral administration to man , 1979, European Journal of Clinical Pharmacology.

[30]  Hossein Afarideh,et al.  Journal of Pharmacy & Pharmaceutical Sciences A Publication of the Canadian Society for Pharmaceutical Sciences Société canadienne des sciences pharmaceutiques , 2000 .

[31]  A. Somogyi,et al.  Effect of cimetidine on renal and hepatic drug elimination: Studies with triamterene , 1986, Clinical pharmacology and therapeutics.

[32]  A. Somogyi,et al.  Reduction of metformin renal tubular secretion by cimetidine in man. , 1987, British journal of clinical pharmacology.

[33]  S. Chong,et al.  Evaluation of Permeability and P-glycoprotein Interactions: Industry Outlook , 2008 .

[34]  Geraldine Rauch,et al.  Trimethoprim-metformin interaction and its genetic modulation by OCT2 and MATE1 transporters. , 2013, British journal of clinical pharmacology.

[35]  E. Burchard,et al.  Effect of genetic variation in the organic cation transporter 2 on the renal elimination of metformin , 2009, Pharmacogenetics and genomics.

[36]  R. Day,et al.  Clinical Pharmacokinetics of Metformin , 2011, Clinical pharmacokinetics.

[37]  Alex Avdeef,et al.  Absorption and Drug Development: Solubility, Permeability, and Charge State , 2003 .

[38]  U. Lee,et al.  Pharmacokinetic interaction between itraconazole and metformin in rats: competitive inhibition of metabolism of each drug by each other via hepatic and intestinal CYP3A1/2 , 2010, British journal of pharmacology.

[39]  J. Villeneuve,et al.  Cimetidine Kinetics and Dynamics in Patients with Severe Liver Disease , 2007, Hepatology.

[40]  S. Wright,et al.  Renal transport of organic anions and cations. , 2011, Comprehensive Physiology.

[41]  M. Uusitupa,et al.  The pharmacokinetics of metformin: a comparison of the properties of a rapid-release and a sustained-release preparation. , 1983, International journal of clinical pharmacology, therapy, and toxicology.

[42]  R. Neubert,et al.  Drug specificity and intestinal membrane localization of human organic cation transporters (OCT). , 2005, Biochemical pharmacology.

[43]  G. Bowers,et al.  Metformin's Intrinsic Blood-to-Plasma Partition Ratio (B/P): Reconciling the Perceived High In Vivo B/P > 10 with the In Vitro Equilibrium Value of Unity , 2015, The Journal of Pharmacology and Experimental Therapeutics.

[44]  Y. Sugiyama,et al.  Transporters in Drug Development , 2013, AAPS Advances in the Pharmaceutical Sciences Series.

[45]  H. Kusuhara,et al.  Potent and Specific Inhibition of mMate1-Mediated Efflux of Type I Organic Cations in the Liver and Kidney by Pyrimethamine , 2010, Journal of Pharmacology and Experimental Therapeutics.

[46]  G. Lee,et al.  Influence of culture passages on growth kinetics and adenovirus vector production for gene therapy in monolayer and suspension cultures of HEK 293 cells , 2004, Applied Microbiology and Biotechnology.

[47]  Pentikäinen Pj.  Bioavailability of metformin. Comparison of solution, rapidly dissolving tablet, and three sustained release products. , 1986 .

[48]  Maria M. Posada,et al.  Prediction of Renal Transporter Mediated Drug-Drug Interactions for Pemetrexed Using Physiologically Based Pharmacokinetic Modeling , 2015, Drug Metabolism and Disposition.

[49]  Lei Zhang,et al.  Towards Quantitation of the Effects of Renal Impairment and Probenecid Inhibition on Kidney Uptake and Efflux Transporters, Using Physiologically Based Pharmacokinetic Modelling and Simulations , 2014, Clinical Pharmacokinetics.

[50]  J. A. Carrillo,et al.  Comparative in vitro and in vivo inhibition of cytochrome P450 CYP1A2, CYP2D6, and CYP3A by H2‐receptor antagonists , 1999, Clinical pharmacology and therapeutics.

[51]  P. Pentikäinen.  Bioavailability of metformin. Comparison of solution, rapidly dissolving tablet, and three sustained release products. , 1986, International journal of clinical pharmacology, therapy, and toxicology.

[52]  G. Levy,et al.  Pharmacokinetics of Metformin Gastric‐Retentive Tablets in Healthy Volunteers , 2001, Journal of clinical pharmacology.

[53]  A. Rosén,et al.  Bioavailability and pharmacokinetics of cimetidine , 1979, European Journal of Clinical Pharmacology.

[54]  T. Salvatore,et al.  Reduction of the acute bioavailability of metformin by the α‐glucosidase inhibitor acarbose in normal man , 1994, European journal of clinical investigation.

[55]  HighWire Press,et al.  American journal of physiology. Cell physiology , 1977 .

[56]  A. Gibson,et al.  Conjunctive therapy of cisplatin with the OCT2 inhibitor cimetidine: influence on antitumor efficacy and systemic clearance , 2013, Clinical pharmacology and therapeutics.

[57]  D. Thakker,et al.  Mechanisms Underlying Saturable Intestinal Absorption of Metformin , 2008, Drug Metabolism and Disposition.

[58]  P Timmins,et al.  In vitro-in vivo correlation (IVIVC) models for metformin after administration of modified-release (MR) oral dosage forms to healthy human volunteers. , 2001, Journal of pharmaceutical sciences.

[59]  Satohiro Masuda,et al.  Involvement of Human Multidrug and Toxin Extrusion 1 in the Drug Interaction between Cimetidine and Metformin in Renal Epithelial Cells , 2009, Journal of Pharmacology and Experimental Therapeutics.

[60]  H. Barton,et al.  Prediction of Pharmacokinetics and Drug–Drug Interactions When Hepatic Transporters are Involved , 2014, Clinical Pharmacokinetics.

[61]  Y Kumagai,et al.  Effects of a MATE Protein Inhibitor, Pyrimethamine, on the Renal Elimination of Metformin at Oral Microdose and at Therapeutic Dose in Healthy Subjects , 2011, Clinical pharmacology and therapeutics.

[62]  W. Kirch,et al.  Cisapride-cimetidine interaction: enhanced cisapride bioavailability and accelerated cimetidine absorption. , 1989, Therapeutic drug monitoring.

[63]  Masahiro Okuda,et al.  Metformin Transport by Renal Basolateral Organic Cation Transporter hOCT2 , 2005, Pharmaceutical Research.

[64]  Priyadaranjan. Ray.  Complex Compounds of Biguanides and Guanylureas with Metallic Elements. , 1961 .

[65]  A. Sparreboom,et al.  Uptake Carriers and Oncology Drug Safety , 2014, Drug Metabolism and Disposition.

[66]  A Rostami-Hodjegan,et al.  Absolute abundance and function of intestinal drug transporters: a prerequisite for fully mechanistic in vitro-in vivo extrapolation of oral drug absorption. , 2013, Biopharmaceutics & drug disposition.

[67]  Brian Tomlinson,et al.  OCT2 polymorphisms and in-vivo renal functional consequence: studies with metformin and cimetidine , 2008, Pharmacogenetics and genomics.

[68]  R. Veech,et al.  The resting membrane potential of cells are measures of electrical work, not of ionic currents , 1995, Integrative physiological and behavioral science : the official journal of the Pavlovian Society.

[69]  Roland Gugler,et al.  Influence of phenobarbital treatment on cimetidine kinetics , 2004, European Journal of Clinical Pharmacology.

[70]  S. Soldin,et al.  Ranitidine kinetics and dynamics: II. Intravenous dose studies and comparison with cimetidine , 1981, Clinical pharmacology and therapeutics.

[71]  Lawrence X. Yu,et al.  Biopharmaceutics Applications In Drug Development , 2008 .

[72]  HighWire Press,et al.  The journal of pharmacology and experimental therapeutics , 1909 .

[73]  Hiroshi Omote,et al.  A human transporter protein that mediates the final excretion step for toxic organic cations. , 2005, Proceedings of the National Academy of Sciences of the United States of America.

[74]  W. Stein.  How the kinetic parameters of the simple carrier are affected by an applied voltage. , 1977, Biochimica et biophysica acta.

[75]  Katsuhisa Inoue,et al.  Functional characteristics of two human MATE transporters: kinetics of cimetidine transport and profiles of inhibition by various compounds. , 2010, Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques.

[76]  R. Altman,et al.  Metformin pathways: pharmacokinetics and pharmacodynamics , 2012, Pharmacogenetics and genomics.

[77]  A. Wen,et al.  The effect of lansoprazole, an OCT inhibitor, on metformin pharmacokinetics in healthy subjects , 2013, European Journal of Clinical Pharmacology.

[78]  C. Bailey,et al.  Metformin and the gastrointestinal tract , 2016, Diabetologia.

[79]  H Connor,et al.  Metformin kinetics in healthy subjects and in patients with diabetes mellitus. , 1981, British journal of clinical pharmacology.

[80]  M. Andréjak,et al.  Kinetics of plasma and erythrocyte metformin after acute administration in healthy subjects. , 2003, Diabetes & metabolism.

[81]  H. Kusuhara,et al.  Competitive Inhibition of the Luminal Efflux by Multidrug and Toxin Extrusions, but Not Basolateral Uptake by Organic Cation Transporter 2, Is the Likely Mechanism Underlying the Pharmacokinetic Drug-Drug Interactions Caused by Cimetidine in the Kidney , 2012, Journal of Pharmacology and Experimental Therapeutics.

[82]  P. Lory,et al.  Overexpression of T‐type calcium channels in HEK‐293 cells increases intracellular calcium without affecting cellular proliferation , 2000, FEBS letters.

[83]  Effect of variations in urine pH and flow rate on cimetidine renal disposition in man. , 1985, Biopharmaceutics & drug disposition.

[84]  A. Sparreboom,et al.  Can erlotinib ameliorate cisplatin-induced toxicities? , 2013, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[85]  Lu Gaohua,et al.  Accounting for Transporters in Renal Clearance: Towards a Mechanistic Kidney Model (Mech KiM) , 2013 .

[86]  J. Nezu,et al.  Cloning and characterization of a novel human pH‐dependent organic cation transporter, OCTN1 , 1997, FEBS letters.

[87]  B. Wynne,et al.  The Effect of Dolutegravir on the Pharmacokinetics of Metformin in Healthy Subjects , 2016, Journal of acquired immune deficiency syndromes.

[88]  D. Taylor,et al.  The metabolism and elimination of cimetidine, a histamine H2-receptor antagonist, in the rat, dog, and man. , 1978, Drug metabolism and disposition: the biological fate of chemicals.

[89]  W. J. Westlake,et al.  Bioavailability of cimetidine in man , 1978 .

[90]  A. Somogyi,et al.  Pharmacokinetics and Bioavailability of Cimetidine in Gastric and Duodenal Ulcer Patients , 1980, Clinical pharmacokinetics.

[91]  G. Schäfer,et al.  Interaction of biguanides with mitochondrial and synthetic membranes. , 1972, European journal of biochemistry.

[92]  C. Gillen,et al.  Functional interaction of the K-Cl cotransporter (KCC1) with the Na-K-Cl cotransporter in HEK-293 cells. , 1999, American journal of physiology. Cell physiology.