The Effect of Famotidine, a MATE1-Selective Inhibitor, on the Pharmacokinetics and Pharmacodynamics of Metformin

Clinical Pharmacokinetics

Volumn 55, Issue 6, 2016, Pages 711-721

  Hibma, Jennifer E ^a   Zur, Arik A ^a   Castro, Richard A ^a   Wittwer, Matthias B ^a   Keizer, Ron J ^a   Yee, Sook Wah ^a   Goswami, Srijib ^a   Stocker, Sophie L ^a   Zhang, Xuexiang ^b   Huang, Yong ^b   Brett, Claire M ^a   Savic, Radojka M ^a   Giacomini, Kathleen M ^a  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b Optivia Biotechnology Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CREATININE; FAMOTIDINE; GLUCOSE; METFORMIN; MULTIDRUG AND TOXIN EXTRUSION PROTEIN 1; ANTIDIABETIC AGENT; ANTIULCER AGENT; GLUCOSE BLOOD LEVEL; MATE1 PROTEIN, HUMAN; ORGANIC CATION TRANSPORTER;

ADULT; AREA UNDER THE CURVE; ARTICLE; CLINICAL EVALUATION; CONCENTRATION RESPONSE; CONTROLLED STUDY; CREATININE BLOOD LEVEL; CREATININE URINE LEVEL; CROSSOVER PROCEDURE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG INHIBITION; DRUG POTENTIATION; ENZYME INHIBITION; FEMALE; GLUCOSE BLOOD LEVEL; HUMAN; HUMAN CELL; HUMAN EXPERIMENT; IN VITRO STUDY; IN VIVO STUDY; MALE; MULTIPLE DRUG DOSE; NORMAL HUMAN; ORAL GLUCOSE TOLERANCE TEST; OUTCOME ASSESSMENT; PHARMACODYNAMICS; PHARMACOKINETIC PARAMETERS; PLASMA CONCENTRATION-TIME CURVE; PRIORITY JOURNAL; PROTEIN EXPRESSION; RENAL CLEARANCE; SINGLE DRUG DOSE; TIME TO MAXIMUM PLASMA CONCENTRATION; URINALYSIS; URINARY EXCRETION; ANTAGONISTS AND INHIBITORS; BLOOD; CLINICAL TRIAL; DOSE RESPONSE; URINE; YOUNG ADULT;

ADULT; ANTI-ULCER AGENTS; AREA UNDER CURVE; BLOOD GLUCOSE; CREATININE; CROSS-OVER STUDIES; DOSE-RESPONSE RELATIONSHIP, DRUG; FAMOTIDINE; FEMALE; HUMANS; HYPOGLYCEMIC AGENTS; MALE; METFORMIN; ORGANIC CATION TRANSPORT PROTEINS; YOUNG ADULT;

EID: 84947997758     PISSN: 03125963     EISSN: 11791926     Source Type: Journal    
DOI: 10.1007/s40262-015-0346-3     Document Type: Article

References (54)

1. Hillgren KM, Keppler D, Zur AA, Giacomini KM, Stieger B, Cass CE, et al. Emerging transporters of clinical importance: an update from the International Transporter Consortium. Clin Pharmacol Ther. 2013;94:52–63.
2. Lu M, Symersky J, Radchenko M, Koide A, Guo Y, Nie R, et al. Structures of a Na+-coupled, substrate-bound MATE multidrug transporter. Proc Natl Acad Sci. 2013;110:2099–104.
3. Lu M, Radchenko M, Symersky J, Nie R, Guo Y. Structural insights into H+-coupled multidrug extrusion by a MATE transporter. Nat Struct Mol Biol. 2013;20:1310–7.
4. Damme K, Nies AT, Schaeffeler E, Schwab M. Mammalian MATE (SLC47A) transport proteins: impact on efflux of endogenous substrates and xenobiotics. Drug Metab Rev. 2011;43:499–523.
5. Motohashi H, Inui K. Multidrug and toxin extrusion family SLC47: physiological, pharmacokinetic and toxicokinetic importance of MATE1 and MATE2-K. Mol Aspects Med. 2013;34:661–8.
6. Yonezawa A, Inui K. Importance of the multidrug and toxin extrusion MATE/SLC47A family to pharmacokinetics, pharmacodynamics/toxicodynamics and pharmacogenomics. Br J Pharmacol. 2011;164:1817–25.
7. Tanihara Y, Masuda S, Sato T, Katsura T, Ogawa O, Inui K. Substrate specificity of MATE1 and MATE2-K, human multidrug and toxin extrusions/H+-organic cation antiporters. Biochem Pharmacol. 2007;74:359–71.
8. Masuda S, Terada T, Yonezawa A, Tanihara Y, Kishimoto K, Katsura T, et al. Identification and functional characterization of a new human kidney-specific H+/organic cation antiporter, kidney-specific multidrug and toxin extrusion 2. J Am Soc Nephrol. 2006;17:2127–35.
9. Otsuka M, Matsumoto T, Morimoto R, Arioka S, Omote H, Moriyama Y. A human transporter protein that mediates the final excretion step for toxic organic cations. Proc Natl Acad Sci. 2005;102:1–6.
10. Lee JH, Lee JE, Kim Y, Lee H, Jun H, Lee S. Multidrug and toxic compound extrusion protein-1 (MATE1/SLC47A1) is a novel flavonoid transporter. J Agric Food Chem. 2014;62:9690–8.
11. Levey AS, Perrone RD, Madias NE. Serum creatinine and renal function. Annu Rev Med. 1988;39:465–90.
12. Lepist E-I, Zhang X, Hao J, Huang J, Kosaka A, Birkus G, et al. Contribution of the organic anion transporter OAT2 to the renal active tubular secretion of creatinine and mechanism for serum creatinine elevations caused by cobicistat. Kidney Int. 2014;86:350–7.
13. Imamura Y, Murayama N, Okudaira N, Kurihara A, Okazaki O, Izumi T, et al. Prediction of fluoroquinolone-induced elevation in serum creatinine levels: a case of drug–endogenous substance interaction involving the inhibition of renal secretion. Clin Pharmacol Ther. 2009;89:81–8.
14. Gong L, Goswami S, Giacomini KM, Altman RB, Klein TE. Metformin pathways. Pharmacogenet Genomics. 2012;22:820–7.
15. Graham GG, Punt J, Arora M, Day RO, Doogue MP, Duong JK, et al. Clinical pharmacokinetics of metformin. Clin Pharmacokinet. 2011;50:81–98.
16. Tsuda M, Terada T, Mizuno T, Katsura T, Shimakura J, Inui K. Targeted disruption of the multidrug and toxin extrusion 1 (mate1) gene in mice reduces renal secretion of metformin. Mol Pharmacol. 2009;75:1280–6.
17. Toyama K, Yonezawa A, Masuda S, Osawa R, Hosokawa M, Fujimoto S, et al. Loss of multidrug and toxin extrusion 1 (MATE1) is associated with metformin-induced lactic acidosis. Br J Pharmacol. 2012;166:1183–91.
18. Becker ML, Visser LE, van Schaik RHN, Hofman A. Genetic variation in the multidrug and toxin extrusion 1 transporter protein influences the glucose-lowering effect of metformin in patients with diabetes: a preliminary study. Diabetes. 2009;58:745–9.
19. Tkáč I, Klimčáková L, Javorský M, Fabianová M, Schroner Z, Hermanová H, et al. Pharmacogenomic association between a variant in SLC47A1 gene and therapeutic response to metformin in type 2 diabetes. Diabetes Obes Metab. 2013;15:189–91.
20. Becker ML, Visser LE, van Schaik RHN, Hofman A, Uitterlinden AG, Stricker BHC. Interaction between polymorphisms in the OCT1 and MATE1 transporter and metformin response. Pharmacogenet Genomics. 2010;20:38–44.
21. Jablonski KA, McAteer JB, de Bakker PIW, Franks PW, Pollin TI, Hanson RL, et al. Common variants in 40 genes assessed for diabetes incidence and response to metformin and lifestyle intervention in the Diabetes Prevention Program. Diabetes. 2010;59:2672–81.
22. Stocker SL, Morrissey KM, Yee SW, Castro RA, Xu L, Dahlin A, et al. The effect of novel promoter variants in MATE1 and MATE2 on the pharmacokinetics and pharmacodynamics of metformin. Clin Pharmacol Ther. 2012;93:186–94.
23. Kusuhara H, Ito S, Kumagai Y, Jiang M, Shiroshita T, Moriyama Y, 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. Clin Pharmacol Ther. 2011;89:837–44.
24. Ito S, Kusuhara H, Kuroiwa Y, Wu C, Moriyama Y, Inoue K, et al. Potent and specific inhibition of mMate1-mediated efflux of type i organic cations in the liver and kidney by pyrimethamine. J Pharmacol Exp Ther. 2010;333:341–50.
25. Somogyi A, Stockley C, Keal J, Rolan P, Bochner F. Reduction of metformin renal tubular secretion by cimetidine in man. Br J Clin Pharmacol. 1987;23:545–51.
26. Ha Choi J, Wah Yee S, Kim MJ, Nguyen L, Ho Lee J, Kang J-O, et al. Identification and characterization of novel polymorphisms in the basal promoter of the human transporter, MATE1. Pharmacogenet Genomics. 2009;19:770–80.
27. Wittwer MB, Zur AA, Khuri N, Kido Y, Kosaka A, Zhang X, et al. Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. J Med Chem. 2013;56:781–95.
28. Pepcid label. Merck & Co., Inc.; 2011. http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019462s037lbl.pdf.
29. Yeh KC, Chremos AN, Lin JH, Constanzer ML, Kanovsky SM, Hucker HB, et al. Single-dose pharmacokinetics and bioavailability of famotidine in man. Results of multicenter collaborative studies. Biopharm Drug Dispos. 1987;8:549–60.
30. Dowling TC, Frye RF, Fraley DS, Matzke GR. Characterization of tubular functional capacity in humans using para-aminohippurate and famotidine. Kidney Int. 2001;59:295–303.
31. Chremos AN. Clinical pharmacology of famotidine: a summary. J Clin Gastroenterol. 1987;9(Suppl 2):7–12.
32. Kroemer H, Klotz U. Pharmacokinetics of famotidine in man. Int J Clin Pharmacol Ther Toxicol. 1987;25:458–63.
33. Shu Y, Brown C, Castro RA, Shi RJ, Lin ET, Owen RP, et al. Effect of genetic variation in the organic cation transporter 1, OCT1, on metformin pharmacokinetics. Clin Pharmacol Ther. 2007;83:273–80.
34. Lin JH, Los LE, Ulm EH, Duggan DE. Kinetic studies on the competition between famotidine and cimetidine in rats. Evidence of multiple renal secretory systems for organic cations. Drug Metab Dispos. 1988;16:52–6.
35. Dowling T, Frye R, Fraley D, Matzke G. Characterization of tubular functional capacity in humans using para-aminohippurate and famotidine. Kidney Int. 2001;59:295–303.
36. Levey AS, Stevens LA, Schmid CH, Zhang YL, Castro AF, Feldman HI, et al. A new equation to estimate glomerular filtration rate. Ann Intern Med. 2009;150:604–12.
37. Goswami S, Yee SW, Stocker S, Mosley JD, Kubo M, Castro R, et al. Genetic variants in transcription factors are associated with the pharmacokinetics and pharmacodynamics of metformin. Clin Pharmacol Ther. 2014;96:370–9.
38. Pentikäinen PJ, Neuvonen PJ, Penttilä A. Pharmacokinetics of metformin after intravenous and oral administration to man. Eur J Clin Pharmacol. 1979;16:195–202.
39. Sambol NC, Chiang J, O’Conner M, Liu CY, Lin ET, Goodman AM, et al. Pharmacokinetics and Pharmacodynamics of metformin in healthy subjects and patients with noninsulin-dependent diabetes mellitus. J Clin Pharmacol. 1996;36:1012–21.
40. Wang Z-J, Yin OQP, Tomlinson B, Chow MSS. OCT2 polymorphisms and in-vivo renal functional consequence: studies with metformin and cimetidine. Pharmacogenet Genomics. 2008;18:637–45.
41. Stepensky D, Friedman M, Srour W, Raz I, Hoffman A. Preclinical evaluation of pharmacokinetic–pharmacodynamic rationale for oral CR metformin formulation. J Control Release. 2001;71:107–15.
42. Zamek-Gliszczynski MJ, Bao JQ, Day JS, Higgins JW. Metformin sinusoidal efflux from the liver is consistent with negligible biliary excretion and absence of enterohepatic cycling. Drug Metab Dispos. 2013;41:1967–71.
43. Han TK, Proctor WR, Costales CL, Cai H, Everett RS, Thakker DR. Four cation-selective transporters contribute to apical uptake and accumulation of metformin in Caco-2 cell monolayers. J Pharmacol Exp Ther. 2015;352:519–28.
44. Nakamichi N, Shima H, Asano S, Ishimoto T, Sugiura T, Matsubara K, et al. Involvement of carnitine/organic cation transporter OCTN1/SLC22A4 in gastrointestinal absorption of metformin. J Pharm Sci. 2013;102:3407–17.
45. Zhou M, Xia L, Wang J. Metformin transport by a newly cloned proton-stimulated organic cation transporter (plasma membrane monoamine transporter) expressed in human intestine. Drug Metab Dispos. 2007;35:1956–62.
46. Hume WE, Shingaki T, Takashima T, Hashizume Y, Okauchi T, Katayama Y, et al. The synthesis and biodistribution of [(11)C]metformin as a PET probe to study hepatobiliary transport mediated by the multi-drug and toxin extrusion transporter 1 (MATE1) in vivo. Bioorg Med Chem. 2013;21:7584–90.
47. Li Q, Guo D, Dong Z, Zhang W, Zhang L, Huang S-M, et al. Ondansetron can enhance cisplatin-induced nephrotoxicity via inhibition of multiple toxin and extrusion proteins (MATEs). Toxicol Appl Pharmacol. 2013;273:100–9.
48. Somogyi A, McLean A, Heinzow B. Cimetidine-procainamide pharmacokinetic interaction in man: Evidence of competition for tubular secretion of basic drugs. Eur J Clin Pharmacol. 1983;25:339–45.
49. Van Crugten J, Bochner F, Keal J, Somogyi A. Selectivity of the cimetidine-induced alterations in the renal handling of organic substrates in humans. Studies with anionic, cationic and zwitterionic drugs. J Pharmacol Exp Ther. 1986;236:481–7.
50. Yasui-Furukori N, Uno T, Sugawara K, Tateishi T. Different effects of three transporting inhibitors, verapamil, cimetidine, and probenecid, on fexofenadine pharmacokinetics. Clin Pharmacol Ther. 2005;77:17–23.
51. Ray AS. Creatinine and renal transporters. Endogenous biomarkers: mother nature’s guide to predicting drug–drug interactions. creatine and renal transporters. AAPS annual meeting and exposition; 2–6 Nov 2014: San Diego (CA).
52. Wang D-S, Jonker JW, Kato Y, Kusuhara H, Schinkel AH, Sugiyama Y. Involvement of organic cation transporter 1 in hepatic and intestinal distribution of metformin. J Pharmacol Exp Ther. 2002;302:510–5.
53. Motohashi H, Uwai Y, Hiramoto K, Okuda M, Inui K-I. Different transport properties between famotidine and cimetidine by human renal organic ion transporters (SLC22A). Eur J Pharmacol. 2004;503:25–30.
54. Xia L, Engel K, Zhou M, Wang J. Membrane localization and pH-dependent transport of a newly cloned organic cation transporter (PMAT) in kidney cells. Am J Physiol Renal Physiol. 2007;292:F682–90.