Potassium-competitive acid blockers: Advanced therapeutic option for acid-related diseases

Pharmacology and Therapeutics

Volumn 168, Issue , 2016, Pages 12-22

  Inatomi, Nobuhiro ^a   Matsukawa, Jun ^a   Sakurai, Yuuichi ^a   Otake, Kazuyoshi ^a  

^a TAKEDA PHARMACEUTICAL COMPANY LIMITED   (Japan)

Author keywords

Acid related diseases; Gastric acid secretion; H2 receptor; Peptic ulcer; Potassium competitive acid blocker; Proton pump inhibitor

Indexed keywords

ANTACID AGENT; POTASSIUM COMPETITIVE ACID BLOCKER; PROTEIN INHIBITOR; PROTON PUMP INHIBITOR; RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG; GASTROINTESTINAL AGENT; HISTAMINE H2 RECEPTOR ANTAGONIST; POTASSIUM;

ACID RELATED DISEASE; ADVERSE DRUG REACTION; AREA UNDER THE CURVE; ARTICLE; BACTERIAL CLEARANCE; COMPARATIVE EFFECTIVENESS; DIGESTIVE SYSTEM DISEASE; DRUG BIOAVAILABILITY; DRUG DISPOSITION; DRUG EFFICACY; DRUG MECHANISM; DRUG SAFETY; HALF LIFE TIME; HELICOBACTER PYLORI; HUMAN; MAXIMUM PLASMA CONCENTRATION; PHARMACODYNAMICS; PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL (TOPIC); REFLUX ESOPHAGITIS; STOMACH ACID SECRETION; TIME TO MAXIMUM PLASMA CONCENTRATION; ANIMAL; COMPLICATION; DRUG DESIGN; GASTROESOPHAGEAL REFLUX; HELICOBACTER INFECTIONS; ISOLATION AND PURIFICATION; METABOLISM; PATHOPHYSIOLOGY; PEPTIC ULCER; SECRETION (PROCESS); STOMACH ACID;

ANIMALS; DRUG DESIGN; GASTRIC ACID; GASTROESOPHAGEAL REFLUX; GASTROINTESTINAL AGENTS; HELICOBACTER INFECTIONS; HELICOBACTER PYLORI; HISTAMINE H2 ANTAGONISTS; HUMANS; PEPTIC ULCER; POTASSIUM; PROTON PUMP INHIBITORS;

EID: 84994086942     PISSN: 01637258     EISSN: 1879016X     Source Type: Journal    
DOI: 10.1016/j.pharmthera.2016.08.001     Document Type: Article

References (130)

1. Abelö, A., Andersson, T.B., Antonsson, M., Naudot, A.K., Skånberg, I., Weidolf, L., Stereoselective metabolism of omeprazole by human cytochrome P450 enzymes. Drug Metab Dispos 28 (2000), 966–972.
2. Andersson, K., Carlsson, E., Potassium-competitive acid blockade: a new therapeutic strategy in acid-related diseases. Pharmacol Ther 108 (2005), 294–307.
3. Andersson, T., Hassan-Alin, M., Hasselgren, G., Röhss, K., Weidolf, L., Pharmacokinetic studies with esomeprazole, the (S)-isomer of omeprazole. Clin Pharmacokinet 40 (2001), 411–426.
4. +-ATPase. J Biol Chem 275 (2000), 8324–8330.
5. Ash, A.S.F., Schild, H.O., Receptors mediating some actions of histamine. Br J Pharmacol Chemother 27 (1966), 427–439.
6. Ashida, K., Sakurai, Y., Nishimura, A., Kudou, K., Hiramatsu, N., Umegaki, E., et al. Randomised clinical trial: a dose-ranging study of vonoprazan, a novel potassium-competitive acid blocker, vs. lansoprazole for the treatment of erosive oesophagitis. Aliment Pharmacol Ther 42 (2015), 685–695.
7. Ashida, K., Sakurai, Y., Hori, T., Nishimura, A., Hiramatsu, N., Umegaki, E., Iwakiri, K., Randomised clinical trial: vonoprazan, a novel potassium-competitive acid blocker, vs. lansoprazole for the healing of erosive oesophagitis. Aliment Pharmacol Ther 43 (2016), 240–251.
8. Beil, W., Hackbarth, I., Sewing, K.F., Mechanism of gastric antisecretory effect of SCH28080. Br J Pharmacol 88 (1986), 19–23.
9. +-ATPase in the rat heart. Acta Physiol Scand 179 (2003), 251–262.
10. Bell, N.J., Burget, D., Howden, C.W., Wilkinson, J., Hunt, R.H., Appropriate acid suppression for the management of gastro-oesophageal reflux disease. Digestion 51:Suppl. 1 (1992), 59–67.
11. Berg, A.L., Böttcher, G., Andersson, K., Carlsson, E., Lindström, A.K., Huby, R., et al. Early stellate cell activation and veno-occlusive-disease (VOD)-like hepatotoxicity in dogs treated with AR-H047108, an imidazopyridine proton pump inhibitor. Toxicol Pathol 36 (2008), 727–737.
12. +-adenosinetriphosphatase. Biochemistry 32 (1993), 2345–2355.
13. Bhatt, D.L., Cryer, B.L., Contant, C.F., Cohen, M., Lanas, A., Schnitzer, T.J., et al. Clopidogrel with or without omeprazole in coronary artery disease. N Engl J Med 363 (2010), 1909–1917.
14. 2-receptors. Nature 236 (1972), 385–390.
15. Boyce, M., David, O., Darwin, K., Mitchell, T., Johnston, A., Warrington, S., Single oral doses of netazepide (YF476), a gastrin receptor antagonist, cause dose-dependent, sustained increases in gastric pH compared with placebo and ranitidine in healthy subjects. Aliment Pharmacol Ther 36 (2012), 181–189.
16. 2-receptor antagonist. Br J Pharmacol 53 (1975), 435P–436P.
17. Burget, D.W., Chiverton, S.G., Hunt, R.H., Is there an optimal degree of acid suppression for healing of duodenal ulcers? A model of the relationship between ulcer healing and acid suppression. Gastroenterology 99 (1990), 345–351.
18. Chang, R., Chung, I.S., Park, S.H., Kim, S.K., Choi, S.R., Song, G.A., et al. Phase III clinical trial of revaprazan (revanex R) for gastric ulcer. Korean J Gastrointest Endosc 34 (2007), 312–319.
19. Chey, W.D., Mody, R.R., Izat, E., Patient and physician satisfaction with proton pump inhibitors (PPIs): are there opportunities for improvement?. Dig Dis Sci 55 (2010), 3415–3422.
20. Chiu, P.J., Casciano, C., Tetzloff, G., Long, J.F., Barnett, A., Studies on the mechanisms of the antisecretory and cytoprotective actions of SCH28080. J Pharmacol Exp Ther 226 (1983), 121–125.
21. De Graef, J., Woussen-Colle, M.C., Influence of the stimulation state of the parietal cells on the inhibitory effect of omeprazole on gastric acid secretion in dogs. Gastroenterology 91 (1986), 333–337.
22. Dent, J., Kahrilas, P.J., Hatlebakk, J., Vakil, N., Denison, H., Franzén, S., Lundborg, P., A randomized, comparative trial of a potassium-competitive acid blocker (AZD0865) and esomeprazole for the treatment of patients with nonerosive reflux disease. Am J Gastroenterol 103 (2008), 20–26.
23. Dufresne, M., Seva, C., Fourmy, D., Cholecystokinin and gastrin receptors. Physiol Rev 86 (2006), 805–847.
24. Emerson, C.R., Marzella, N., Dexlansoprazole: a proton pump inhibitor with a dual delayed-release system. Clin Ther 32 (2010), 1578–1596.
25. Ene, M.D., Khan-Daneshmend, T., Roberts, C.J.C., A study of the inhibitory effects of SCH 28080 on gastric secretion in man. Br J Pharmacol 76 (1982), 389–391.
26. +)-ATPase. Nature 290 (1981), 159–161.
27. Feurle, G.E., Effect of rising intragastric pH induced by several antacids on serum gastrin concentrations in duodenal ulcer patients and in a control group. Gastroenterology 68 (1975), 1–7.
28. 2 receptor antagonists on night intragastric acidity in active duodenal ulcer patients?. Am J Gastroenterol 83 (1988), 1371–1375.
29. Forte, J.G., Zhu, L., Apical recycling of the gastric parietal cell H,K-ATPase. Annu Rev Physiol 72 (2010), 273–296.
30. Forte, T.M., Machen, T.E., Forte, J.G., Ultrastructural changes in oxyntic cells associate with secretory function: a membrane-recycling hypothesis. Gastroenterology 73 (1977), 941–955.
31. Frelinger, A.L. III, Lee, R.D., Mulford, D.J., Wu, J., Nudurupati, S., Nigam, A., et al. A randomized, 2-period, crossover design study to assess the effects of dexlansoprazole, lansoprazole, esomeprazole, and omeprazole on the steady-state pharmacokinetics and pharmacodynamics of clopidogrel in healthy volunteers. J Am Coll Cardiol 59 (2012), 1304–1311 Erratum in J Am Coll Cardiol (2012) 60, 566–567.
32. Furuta, T., Shirai, N., Sugimoto, M., Nakamura, A., Hishida, A., Ishizaki, T., Influence of CYP2C19 pharmacogenetic polymorphism on proton pump inhibitor-based therapies. Drug Metab Pharmacokinet 20 (2005), 153–167.
33. +-stimulated ATPase in purified microsomes of bullfrog oxyntic cells. Biochim Biophys Acta 307 (1973), 169–180.
34. +-ATPase. Biochem Pharmacol 73 (2007), 198–205.
35. 2 + concentration in parietal cells depends on adenosine 3′,5′-cyclic monophosphate levels. Gastroenterology 109 (1995), 1060–1067.
36. Hall, K., Perez, G., Anderson, D., Gutierrrez, C., Munson, K., Hersey, S.J., et al. Location of the cabohydrates present in the HK-ATPase vesicles isolated from hog gastric mucosa. Biochemistry 29 (1990), 701–706.
37. Hatlebakk, J.G., Berstad, A., Pharmacokinetic optimization in the treatment of gastro-oesophageal reflux disease. Clin Pharmacokinet 31 (1996), 386–406.
38. Helander, H.F., Hirschowitz, B.I., Quantitative ultrastructural studies on gastric parietal cells. Gastroenterology 63 (1972), 951–961.
39. Helander, H.F., Ramsay, C.H., Regårdh, C.G., Localization of omeprazole and metabolites in the mouse. Scand J Gastroenterol 20:Suppl.108 (1985), 95–104.
40. +-ATPase in human tissue. Scand J Gastroenterol 42 (2007), 1275–1288.
41. Hinkle, K.L., Bane, G.C., Jazayeri, A., Samuelson, L.C., Enhanced calcium signaling and acid secretion in parietal cells isolated from gastrin-deficient mice. Am J Physiol Gastrointest Liver Physiol 284 (2003), G145–G153.
42. Holstein, B., Holmberg, A., Florentzson, M., Aurell Holmberg, A., Andersson, M., Andersson, K., AZD0865, a potassium-competitive acid blocker (P-CAB), provides predictable inhibition of acid secretion with repeated dosing in the dog. Eur J Pharm Sci, 23(Suppl. 1), 2004, S8.
43. Holstein, B., Holmberg, A., Florentzson, M., Aurell Holmberg, A., Andersson, M., Andersson, K., AZD0865 – a new potassium-competitive acid blocker – exhibits maximal gastric antisecretory effects from first dose. Gastroenterology, 126, 2004, A-334 M1437.
44. Hori, Y., Imanishi, A., Matsukawa, J., Tsukimi, Y., Nishida, H., Arikawa, Y. Inatomi, N., 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine monofumarate (TAK-438), a novel and potent potassium-competitive acid blocker for the treatment of acid-related diseases. J Pharmacol Exp Ther 335 (2010), 231–238.
45. Hori, Y., Matsukawa, J., Takeuchi, T., Nishida, H., Kajino, M., Inatomi, N., A study comparing the antisecretory effect of TAK-438, a novel potassium-competitive acid blocker, with lansoprazole in animals. J Pharmacol Exp Ther 337 (2011), 797–804.
46. Howden, C.W., Burget, D.W., Hunt, R.H., A meta-analysis to predict gastric ulcer healing from acid suppression. Gastroenterology, 100, 1991, A3.
47. Howden, C.W., Burget, D.W., Hunt, R.H., Appropriate acid suppression for optimal healing of duodenal ulcer and gastro-oesophageal reflux disease. Scand J Gastroenterol Suppl 201 (1994), 79–82.
48. Hunt, R.H., Importance of pH control in the management of GERD. Arch Intern Med 159 (1999), 649–657.
49. Hunt, R.H., Scarpignato, C., Potassium-competitive acid blockers (P-CABs): are they finally ready for prime time in acid-related diseases?. Clin Transl Gastroenterol, 6, 2015, e119.
50. Hunt, R.H., Armstrong, D., Yaghoobi, M., James, C., Chen, Y., Leonard, J., et al. Predictable prolonged suppression of gastric acidity with a novel proton pump inhibitor, AGN201904-Z. Aliment Pharmacol Ther 28 (2008), 187–199.
51. Jenkins, H., Sakurai, Y., Nishimura, A., Okamoto, H., Hibberd, M., Jenkins, R., et al. Randomised clinical trial: safety, tolerability, pharmacokinetics and pharmacodynamics of repeated doses of TAK-438 (vonoprazan), a novel potassium-competitive acid blocker, in healthy male subjects. Aliment Pharmacol Ther 41 (2015), 636–648.
52. Kagami, T., Sahara, S., Ichikawa, H., Uotani, T., Yamade, M., Sugimoto, M., et al. Potent acid inhibition by vonoprazan in comparison with esomeprazole, with reference to CYP2C19 genotype. Aliment Pharmacol Ther 43 (2016), 1048–1059.
53. Kahrilas, P.J., Dent, J., Lauritsen, K., Malfertheiner, P., Denison, H., Franzén, S., Hasselgren, G., A randomized, comparative study of three doses of AZD0865 and esomeprazole for healing of reflux esophagitis. Clin Gastroenterol Hepatol 5 (2007), 1385–1391.
54. Kanai, Y., Nohara, A., Honda, H., Kanno, M., & Sanno, Y. (1969) inventors, Takeda Chemical Ind. Ltd., assignee. Process for producing thioamide derivatives. Japanese patent application, 1969 July (Japanese Patent Notification 1972; 47-41902).
55. Kanno, M., Narumi, S., Hirata, T., Gomaibashi, K., Kanai, Y., Nohara, A., Sanno, Y., Inhibition of the gastric secretion in the rat by thioacetamide derivatives. J Takeda Res Lab 32 (1973), 181–187.
56. +)-ATPase. Biochem Pharmacol 37 (1988), 2231–2236.
57. +)-ATPase. Biochem Pharmacol 42 (1991), 123–130.
58. +)-ATPase. J Biol Chem 264 (1989), 5545–5551.
59. Kim, H.K., Park, S.H., Cheung, D.Y., Cho, Y.S., Kim, J.I., Kim, S.S., et al. Clinical trial: inhibitory effects of revaprazan on gastric acid secretion in healthy male subjects. J Gastroenterol Hepatol 25 (2010), 1618–1625.
60. Kleinman, L., McIntosh, E., Ryan, M., Schmier, J., Crawley, J., Lock, R.G., et al. Willingness to pay for complete symptom relief of gastroesophageal reflux disease. Arch Intern Med 162 (2002), 1361–1366.
61. +-ATPase isoforms in human kidney. Am J Physiol Renal Physiol 281 (2001), F763–F768.
62. Kubo, K., Oda, K., Kaneko, T., Satoh, H., Nohara, A., Synthesis of 2-[[(4-fluoroalkoxy-2-pyridyl)methy]sulfiny]-1H-benzimidazoles as antiulcer agents. Chem Pharm Bull 38 (1990), 2853–2858.
63. Kukulka, M., Eisenberg, C., Nudurupati, S., Comparator pH study to evaluate the single-dose pharmacodynamics of dual delayed-release dexlansoprazole 60 mg and delayed-release esomeprazole 40 mg. Clin Exp Gastroenterol 4 (2011), 213–220.
64. Kuo, C.H., Lu, C.Y., Shih, H.Y., Liu, C.J., Wu, M.C., Hu, H.M., et al. CYP2C19 polymorphism influences Helicobacter pylori eradication. World J Gastroenterol 20 (2014), 16029–16036.
65. Lambrecht, N.W.G., Yakubov, I., Scott, D., Sachs, G., Identification of the K efflux channel coupled to the gastric H-K-ATPase during acid secretion. Physiol Genomics 21 (2005), 81–91.
66. Lee, R.D., Mulford, D., Wu, J., Atkinson, S.N., The effect of time-of-day dosing on the pharmacokinetics and pharmacodynamics of dexlansoprazole MR: evidence for dosing flexibility with a dual delayed release proton pump inhibitor. Aliment Pharmacol Ther 31 (2010), 1001–1011.
67. Lindberg, P., Nordberg, P., Alminger, T., Brändström, A., Wallmark, B., The mechanism of action of the gastric acid secretion inhibitor omeprazole. J Med Chem 29 (1986), 1327–1329.
68. Lundell, L., The physiological background behind and course of development of the first proton pump inhibitor. Scand J Gastroenterol 50 (2015), 680–684.
69. +)-ATPase. Biochem Biophys Res Commun 157 (1988), 203–209.
70. Malen, C.E., Danree, B.H., New thiocarboxamides derivatives with specific gastric antisecretory properties. J Med Chem 14 (1971), 244–246.
71. Malfertheiner, P., Link, A., Selgrad, M., Helicobacter pylori: perspectives and time trends. Nat Rev Gastroenterol Hepatol 11 (2014), 628–638.
72. Maradey-Romero, C., Fass, R., New and future drug development for gastroesophageal reflux disease. J Neurogastroenterol Motil 20 (2014), 6–16.
73. Marshall, B.J., Warren, J.R., Unidentified curved bacilli in the stomach of patients with gastritis and peptic ulceration. Lancet 1 (1984), 1311–1315.
74. Matsukawa, J., Hori, Y., Nishida, H., Kajino, M., Inatomi, N., A comparative study on the modes of action of TAK-438, a novel potassium-competitive acid blocker, and lansoprazole in primary cultured rabbit gastric glands. Biochem Pharmacol 81 (2011), 1145–1151.
75. Matsukawa, J., Kogame, A., Tagawa, Y., Inatomi, N., Radiographic localization study of a novel potassium-competitive acid blocker, vonoprazan, in the rat gastric mucosa. Dig Dis Sci 61 (2016), 1888–1894.
76. McCabe, R.D., Young, D.B., Evidence of a K(+)-H(+)-ATPase in vascular smooth muscle cells. Am J Physiol Heart Circ Physiol 262 (1992), H1955–H1958.
77. Mejia, A., Kraft, W.K., Acid peptic diseases: pharmacological approach to treatment. Expert Rev Clin Pharmacol 2 (2009), 295–314.
78. +-ATPase. J Biol Chem 265 (1990), 5030–5036.
79. Murakami, K., Sakurai, Y., Shiino, M., Funao, N., Nishimura, A., Asaka, M., Vonoprazan, a novel potassium-competitive acid blocker, as a component of first-line and second-line therapy for Helicobacter pylori eradication: a phase III, randomized, double-blind study. Gut 65 (2016), 1439–1446.
80. +)-ATPase activity in canine gastric microsomes and acid formation in isolated canine parietal cells. Biochem Pharmacol 42 (1991), 1875–1878.
81. +)-adenosine triphosphatase by the proton pump inhibitor AG-1749. J Pharmacol Exp Ther 248 (1989), 799–805.
82. +-ATPase in gastric parietal cells from mice. Am J Physiol Gastrointest Liver Physiol 304 (2013), G157–G166.
83. Nilsson, C., Albrektson, E., Rydholm, H., Rohss, K., Hassan-Alin, M., Hasselgren, G., Tolerability, pharmacokinetics and effects on gastric acid secretion after single oral doses of the potassium-competitive acid blocker AZD0865 in healthy male subjects. Gastroenterology, 128(4 Suppl. 2), 2005, A528.
84. Nishida, A., Miyata, K., Tsutsumi, R., Yuki, H., Akuzawa, S., Kobayashi, A., et al. Pharmacological profile of (R)-1-[2,3-dihydro-1-(2′-methylphenacyl)-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo. J Pharmacol Exp Ther 269 (1994), 725–731.
85. Olbe, L., Carlsson, E., Lindberg, P., A proton-pump inhibitor expedition: the case histories of omeprazole and esomeprazole. Nat Rev Drug Discov 2 (2003), 132–139.
86. Park, S., Lee, S., Song, K., Lee, B., Kang, H., Kang, J., The pharmacological properties of a novel acid pump antagonist, YH1885. Gut, 52(Suppl. VI), 2003, A62.
87. Parsons, M.E., Keeling, D.J., Novel approaches to the pharmacological blockade of gastric acid secretion. Expert Opin Investig Drugs 14 (2005), 411–421.
88. Pendley, C.E., Fitzpatrick, L.R., Capolino, A.J., Davis, M.A., Esterline, N.J., Jakubowska, A., et al. RP 73870, a gastrin/cholecystokinin-B receptor antagonist with potent anti-ulcer activity in the rat. J Pharmacol Exp Ther 273 (1995), 1015–1022.
89. Piche, T., Galmiche, J.P., Pharmacological targets in gastro-oesophageal reflux disease. Basic Clin Pharmacol Toxicol 97 (2005), 333–341.
90. +/ATP stoichiometry. J Biol Chem 257 (1982), 6296–6299.
91. +-transporting ATPase. Proc Natl Acad Sci U S A 87 (1990), 6767–6771.
92. + ATPase on cell volume, intracellular pH and migration of human polymorphonuclear leucocytes. Br J Pharmacol 124 (1998), 627–638.
93. Sachs, G., Improving on PPI-based therapy of GORD. Eur J Gastroenterol Hepatol 13:Suppl. 1 (2001), S35–S41.
94. + pump in plasma membranes of hog stomach. J Biol Chem 251 (1976), 7690–7698.
95. Sachs, G., Scott, D.R., Wen, Y., Gastric infection by Helicobacter pylori. Curr Gastroenterol Rep 13 (2011), 540–546.
96. Sachs, G., Shin, J.M., Besancon, M., Prinz, C., The continuing development of gastric acid pump inhibitors. Aliment Pharmacol Ther 7:Suppl. 1 (1993), 4–12 discussion 29-31.
97. Sachs, G., Shin, J.M., Howden, C.W., Review article: the clinical pharmacology of proton pump inhibitors. Aliment Pharmacol Ther 23:Suppl. 2 (2006), 2–8.
98. Sachs, G., Shin, J.M., Hunt, R.H., Novel approaches to inhibition of gastric acid secretion. Curr Gastroenterol Rep 12 (2010), 437–447.
99. Sachs, G., Shin, J.M., Munson, K., Scott, D.R., Gastric acid-dependent diseases: a twentieth-century revolution. Dig Dis Sci 59 (2014), 1358–1369.
100. Sakurai, Y., Mori, Y., Okamoto, H., Nishimura, A., Komura, E., Araki, T., Shiramoto, M., Acid-inhibitory effects of vonoprazan 20 mg compared with esomeprazole 20 mg or rabeprazole 10 mg in healthy adult male subjects — a randomised open-label cross-over study. Aliment Pharmacol Ther 42 (2015), 719–730.
101. Sakurai, Y., Nishimura, A., Kennedy, G., Hibberd, M., Jenkins, R., Okamoto, H., et al. Safety, tolerability, pharmacokinetics and pharmacodynamics of single rising TAK-438 (vonoprazan) doses in healthy male Japanese/non-Japanese subjects. Clin Transl Gastroenterol, 6, 2015, e94.
102. Satoh, H., Discovery and development of proton pump inhibitors. Chiba, T., Malfertheiner, P., Satoh, H., (eds.) Proton Pump Inhibitors: A Balanced View. Basel, Karger Front Gasrointest Res, Vol. 32, 2013, 1–17.
103. Scarpignato, C., Hunt, R.H., Editorial: towards extended acid suppression — the search continues. Aliment Pharmacol Ther 42 (2015), 1027–1029.
104. Scarpignato, C., Kisfalvi, I., D'Amato, M., Varga, G., Effect of dexloxiglumide and spiroglumide, two new CCK-receptor antagonists, on gastric emptying and secretion in the rat: evaluation of their receptor selectivity in vivo. Aliment Pharmacol Ther 10 (1996), 411–419.
105. Schwartz, C., Beitrage zur Pathologie und chirugischen des penetrierenden Magenheschwüren. Mitt Grenzengeb Med Chir (Jena) 5 (1900), 821–848.
106. Scott, D.R., Besancon, M., Sachs, G., Helander, H., Effects of antisecretory agents on parietal cell structure and H/K-ATPase levels in rabbit gastric mucosa in vivo. Dig Dis Sci 39 (1994), 2118–2126.
107. Scott, D.R., Helander, H.F., Hersey, S.J., Sachs, G., The site of acid secretion in the mammalian parietal cell. Biochim Biophys Acta 1146 (1993), 73–80.
108. +-ATPase. Aliment Pharmacol Ther 42 (2015), 1315–1326 Erratum in: Alim Pharmacol Ther 43, 315.
109. Sekiguchi, M., Nagaya, H., Satoh, H., Shino, A., Localization of a novel proton pump inhibitor, lansoprazole, in the gastric mucosa of the rat: a radioautographic study. Acta Histochem Cytochem 25 (1992), 405–410.
110. Shin, J.M., Kim, N., Pharmacokinetics and pharmacodynamics of the proton pump inhibitors. J Neurogastroenterol Motil 19 (2013), 25–35.
111. Shin, J.M., Sachs, G., Gastric H,K-ATPase as a drug target. Dig Dis Sci 51 (2006), 823–833.
112. Shin, J.M., Besancon, M., Prinz, C., Simon, A., Sachs, G., Continuing development of acid pump inhibitors: site of action of pantoprazole. Aliment Pharmacol Ther 8:Suppl. 1 (1994), 11–23.
113. Shin, J.M., Inatomi, N., Munson, K., Strugatsky, D., Tokhtaeva, E., Vagin, O., Sachs, G., Characterization of a novel potassium-competitive acid blocker of the gastric H,K-ATPase, 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine monofumarate (TAK-438). J Pharmacol Exp Ther 339 (2011), 412–420.
114. Shirai, N., Furuta, T., Xiao, F., Kajimura, M., Hanai, H., Ohashi, K., Ishizaki, T., Comparison of lansoprazole and famotidine for gastric acid inhibition during the daytime and night-time in different CYP2C19 genotype groups. Aliment Pharmacol Ther 16 (2002), 837–846.
115. Sippy, B.W., Landmark article may 15, 1915: gastric and duodenal ulcer. Medical cure by an efficient removal of gastric juice corrosion. By Bertram W. Sippy. JAMA 250 (1983), 2192–2197.
116. 14C]-aminopyrine accumulation by isolated canine parietal cells. Gastroenterology 83 (1982), 216–223.
117. Soll, A.H., Wollin, A., Histamine and cyclic AMP in isolated canine parietal cells. Am J Phys 237 (1979), E444–E450.
118. Steel, K., Gastrin and gastrin receptor ligands — a review of recent patent literature. IDrugs 5 (2002), 689–695.
119. B/gastrin receptor antagonist, on acid secretion and experimental duodenal ulcers in rats. Aliment Pharmacol Ther 13 (1999), 87–96.
120. Takinami, Y., Yuki, H., Nishida, A., Akuzawa, S., Uchida, A., Takemoto, Y., et al. YF476 is a new potent and selective gastrin/cholecystokinin-B receptor antagonist in vitro and in vivo. Aliment Pharmacol Ther 11 (1997), 113–120.
121. +-ATPase inhibitor SPI-447. Jpn J Pharmacol 82 (2000), 21–28.
122. Umegaki, E., Iwakiri, K., Hiramatsu, N., Sakurai, Y., Hori, T., Kudou, K., et al. A phase 3, randomized, double-blind, multicenter study to evaluate the efficacy and safety of TAK-438 (10 mg or 20 mg once daily) compared to lansoprazole (15 mg once daily) in a 24-week maintenance treatment for healed erosive esophagitis. Gastroenterology, 146, 2014, S-738 T1052.
123. Vagin, O., Denevich, S., Sachs, G., Plasma membrane delivery of the gastric H,K-ATPase: the role of β-subunit glycosylation. Am J Physiol Cell Physiol 285 (2003), C968–C976.
124. +-ATPase and acid secretion by SCH28080, a substituted pyridyl(1,2a)imidazole. J Biol Chem 262 (1987), 2077–2084.
125. Wedemeyer, R.S., Blume, H., Pharmacokinetic drug interaction profiles of proton pump inhibitors: an update. Drug Saf 37 (2014), 201–211.
126. Wolosin, J.M., Forte, J.G., Kinetic properties of the KCl transport at the secreting apical membrane of the oxyntic cell. J Membr Biol 71 (1983), 195–207.
127. Wurst, W., Hartmann, M., Current status of acid pump antagonists (reversible PPIs). Yale J Biol Med 69 (1996), 233–243.
128. Yao, X., Forte, J.G., Cell biology of acid secretion by the parietal cell. Annu Rev Physiol 65 (2003), 103–131.
129. Yu, K.S., Bae, K.S., Shon, J.H., Cho, J.Y., Yi, S.Y., Chung, J.Y., et al. Pharmacokinetic and pharmacodynamic evaluation of a novel proton pump inhibitor, YH1885, in healthy volunteers. J Clin Pharmacol 44 (2004), 73–82.
130. Yuan, Y., Wang, C.C., Yuan, Y.-H., Hunt, R.H., The proportion of patients who are free of reflux symptoms during the initial days of treatment with proton pump inhibitors (PPIs) in GERD trials: a meta-analysis. Gastroenterology, 134(Suppl. 1), 2008, A-174.