Generic placeholder image

Current Drug Research Reviews


ISSN (Print): 2589-9775
ISSN (Online): 2589-9783

Mini-Review Article

Tegoprazan as a New Remedy for Gastrointestinal Diseases in Comparison with its Therapeutic Predecessors: A Mini-Review

Author(s): Asif Hossain Anik*, Farhana Alam Proma, Pranoy Saha and Sabarni Sarker

Volume 16, Issue 1, 2024

Published on: 10 May, 2023

Page: [11 - 17] Pages: 7

DOI: 10.2174/2589977515666230428140741

Price: $65


Potassium-competitive acid blockers (P-CABs), such as tegoprazan, are a new and diverse class of drugs that can completely block the potassium-binding site of gastric H+/K+ ATPase, potentially overcoming the limitations of proton-pump inhibitors (PPIs). A number of studies have compared the effectiveness as well as the safety profile of tegoprazan to PPIs and other P-CABs for the treatment of gastrointestinal diseases. The current review study evaluates the published works of literature related to clinical pharmacology and clinical trials of tegoprazan for the treatment of diseases related to the gastrointestinal tract. According to the publications included in the study, tegoprazan was found to be safe and well-tolerated and can be used to treat a group of gastrointestinal diseases, including gastroesophageal reflux disease (GERD), non-erosive reflux disease (NERD), and H. pylori combination therapy.

Keywords: Tegoprazan, P-CABs, PPIs, gastrointestinal diseases, GERD, NERD, H. pylori.

Graphical Abstract
Olbe L, Carlsson E, Lindberg P. A proton-pump inhibitor expedition: The case histories of omeprazole and esomeprazole. Nat Rev Drug Discov 2003; 2(2): 132-9.
[] [PMID: 12563304]
Sjöstrand SE, Olbe L, Fellenius E. The discovery and development of the proton pump inhibitor Proton Pump Inhibitors: Milestones in Drug Therapy. Basel: Birkhäuser 1999; pp. 3-20.
Shin JM, Munson K, Vagin O, Sachs G. The gastric HK-ATPase: Structure, function, and inhibition. Pflugers Arch 2009; 457(3): 609-22.
[] [PMID: 18536934]
Sachs G, Shin JM, Howden CW. Review article: The clinical pharmacology of proton pump inhibitors. Aliment Pharmacol Ther 2006; 23(S2): 2-8.
[] [PMID: 16700898]
Otake K, Sakurai Y, Nishida H, et al. Characteristics of the novel potassium-competitive acid blocker vonoprazan fumarate (TAK-438). Adv Ther 2016; 33(7): 1140-57.
[] [PMID: 27287852]
Graham DY, Dore MP. Update on the use of vonoprazan: A competitive acid blocker. Gastroenterology 2018; 154(3): 462-6.
[] [PMID: 29337157]
Akazawa Y, Fukuda D, Fukuda Y. Vonoprazan-based therapy for Helicobacter pylori eradication: Experience and clinical evidence. Therap Adv Gastroenterol 2016; 9(6): 845-52.
[] [PMID: 27803739]
Martinucci I, Blandizzi C, Bodini G, et al. Vonoprazan fumarate for the management of acid-related diseases. Expert Opin Pharmacother 2017; 18(11): 1145-52.
[] [PMID: 28657473]
Takahashi N, Take Y. Tegoprazan, a novel potassium-competitive acid blocker to control gastric acid secretion and motility. J Pharmacol Exp Ther 2018; 364(2): 275-86.
[] [PMID: 29180359]
Chait MM, Mermelstein J, Mermelstein AC. Tegoprazan to treat gastroesophageal reflux disease. Drugs Today 2020; 56(11): 715-21.
[] [PMID: 33332479]
Marcus EA, Pisegna JR. Editorial: Tegoprazan—the newest advance in the management of acid‐related diseases. Aliment Pharmacol Ther 2020; 52(6): 1074-5.
[] [PMID: 33119154]
Yang E, Kim S, Kim B, et al. Night‐time gastric acid suppression by tegoprazan compared to vonoprazan or esomeprazole. Br J Clin Pharmacol 2022; 88(7): 3288-96.
[] [PMID: 35146797]
Sunwoo J, Ji SC, Oh J, et al. Pharmacodynamics of tegoprazan and revaprazan after single and multiple oral doses in healthy subjects. Aliment Pharmacol Ther 2020; 52(11-12): 1640-7.
[PMID: 33131095]
Cho YK, Choi MG, Choi SC, et al. Randomised clinical trial: Tegoprazan, a novel potassium-competitive acid blocker, or lansoprazole in the treatment of gastric ulcer. Aliment Pharmacol Ther 2020; 52(5): 789-97.
[] [PMID: 32701188]
Lindberg P, Brändström A, Wallmark B, Mattsson H, Rikner L, Hoffmann KJ. Omeprazole: The first proton pump inhibitor. Med Res Rev 1990; 10(1): 1-54.
[] [PMID: 2404184]
Bell NJV, Burget D, Howden CW, Wilkinson J, Hunt RH. Appropriate acid suppression for the management of gastro-oesophageal reflux disease. Digestion 1992; 51(1): 59-67.
[] [PMID: 1397746]
Chiba N, De Gara CJ, Wilkinson JM, Hunt RH. Speed of healing and symptom relief in grade II to IV gastroesophageal reflux disease: A meta-analysis. Gastroenterology 1997; 112(6): 1798-810.
[] [PMID: 9178669]
Ashida K. Notes on features and uses of medications used for PPI-resistant GERD, drugs under development and future prospects. Jpn J Med Pharm Sci 2014; 71: 591-6.
Cederberg C, Lind T, Röhss K, Olbe L. Comparison of once-daily intravenous and oral omeprazole on pentagastrin-stimulated acid secretion in duodenal ulcer patients. Digestion 1992; 53(3-4): 171-8.
[] [PMID: 1291405]
Dammann HG, Burkhardt F. Pantoprazole versus omeprazole. Eur J Gastroenterol Hepatol 1999; 11(11): 1277-82.
[] [PMID: 10563540]
Andersson K, Carlsson E. Potassium-competitive acid blockade: A new therapeutic strategy in acid-related diseases. Pharmacol Ther 2005; 108(3): 294-307.
[] [PMID: 16000224]
Bytzer P, Morocutti A, Kennerly P, Ravic M, Miller N. Effect of rabeprazole and omeprazole on the onset of gastro-oesophageal reflux disease symptom relief during the first seven days of treatment. Scand J Gastroenterol 2006; 41(10): 1132-40.
[] [PMID: 16990197]
Peura DA, Riff DS, Snoddy AM, Fennerty MB. Clinical trial: Lansoprazole 15 or 30 mg once daily vs. placebo for treatment of frequent nighttime heartburn in self-treating subjects. Aliment Pharmacol Ther 2009; 30(5): 459-68.
[] [PMID: 19523177]
Piche T, Galmiche JP. Pharmacological targets in gastro-oesophageal reflux disease. Basic Clin Pharmacol Toxicol 2005; 97(6): 333-41.
[] [PMID: 16364047]
Hatlebakk JG, Berstad A. Pharmacokinetic optimisation in the treatment of gastro-oesophageal reflux disease. Clin Pharmacokinet 1996; 31(5): 386-406.
[] [PMID: 9118586]
Kraut JA, Helander KG, Helander HF, Iroezi ND, Marcus EA, Sachs G. Detection and localization of H + -K + -ATPase isoforms in human kidney. Am J Physiol Renal Physiol 2001; 281(4): F763-8.
[] [PMID: 11553523]
Chong E, Ensom MHH. Pharmacogenetics of the proton pump inhibitors: A systematic review. Pharmacotherapy 2003; 23(4): 460-71.
[] [PMID: 12680476]
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 2005; 20(3): 153-67.
[] [PMID: 15988117]
Inatomi N, Matsukawa J, Sakurai Y, Otake K. Potassium-competitive acid blockers: Advanced therapeutic option for acid-related diseases. Pharmacol Ther 2016; 168: 12-22.
[] [PMID: 27514776]
Kleinman L, McIntosh E, Ryan M, et al. Willingness to pay for complete symptom relief of gastroesophageal reflux disease. Arch Intern Med 2002; 162(12): 1361-6.
[] [PMID: 12076234]
Yuan Y, Wang C, Yuan Y, Hunt R. 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 2008; 134(4): A-174.
Hunt RH, Scarpignato C. Potassium-competitive acid blockers (P-CABs): Are they finally ready for prime time in acid-related disease? Clin Transl Gastroenterol 2015; 6(10): e119.
[] [PMID: 26513137]
Chey WD, Mody RR, Izat E. Patient and physician satisfaction with proton pump inhibitors (PPIs): Are there opportunities for improvement? Dig Dis Sci 2010; 55(12): 3415-22.
[] [PMID: 20397047]
Hunt RH, Armstrong D, Yaghoobi M, et al. Predictable prolonged suppression of gastric acidity with a novel proton pump inhibitor, AGN 201904-Z. Aliment Pharmacol Ther 2008; 28(2): 187-99.
[] [PMID: 18445141]
Castell D, Bagin R, Goldlust B, Major J, Hepburn B. Comparison of the effects of immediate-release omeprazole powder for oral suspension and pantoprazole delayed-release tablets on nocturnal acid breakthrough in patients with symptomatic gastro-oesophageal reflux disease. Aliment Pharmacol Ther 2005; 21(12): 1467-74.
[] [PMID: 15948814]
Katz PO, Koch FK, Ballard ED, et al. Comparison of the effects of immediate-release omeprazole oral suspension, delayed-release lansoprazole capsules and delayed-release esomeprazole capsules on nocturnal gastric acidity after bedtime dosing in patients with night-time GERD symptoms. Aliment Pharmacol Ther 2007; 25(2): 197-205.
[] [PMID: 17229243]
Hershcovici T, Jha LK, Fass R, Dexlansoprazole MR. A review. Ann Med 2011; 43(5): 366-74.
[] [PMID: 21366513]
Vakily M, Zhang W, Wu J, Atkinson SN, Mulford D. Pharmacokinetics and pharmacodynamics of a known active PPI with a novel Dual Delayed Release technology, dexlansoprazole MR: A combined analysis of randomized controlled clinical trials. Curr Med Res Opin 2009; 25(3): 627-38.
[] [PMID: 19232037]
Wittbrodt ET, Baum C, Peura DA. Delayed release dexlansoprazole in the treatment of GERD and erosive esophagitis. Clin Exp Gastroenterol 2009; 2: 117-28.
[PMID: 21694835]
Strand DS, Kim D, Peura DA. 25 years of proton pump inhibitors: A comprehensive review. Gut Liver 2017; 11(1): 27-37.
[] [PMID: 27840364]
Beil W, Hackbarth I, Sewing KF. Mechanism of gastric antisecretory effect of SCH 28080. Br J Pharmacol 1986; 88(1): 19-23.
[] [PMID: 3011171]
Wurst W, Hartmann M. Current status of acid pump antagonists (reversible PPIs). Yale J Biol Med 1996; 69(3): 233-43.
[PMID: 9165692]
Oshima T, Miwa H. Potent potassium-competitive acid blockers: A new era for the treatment of acid-related diseases. J Neurogastroenterol Motil 2018; 24(3): 334-44.
[] [PMID: 29739175]
Wallmark B, Briving C, Fryklund J, et al. Inhibition of gastric H+, K+-ATPase and acid secretion by SCH 28080, a substituted pyridyl(1,2a)imidazole. J Biol Chem 1987; 262(5): 2077-84.
[] [PMID: 3029064]
Keeling DJ, Malcolm RC, Laing SM, Ife RJ, Leach CA. SK&F96067 is a reversible, lumenally acting inhibitor of the gastric (H++ K+)-ATPase. Biochem Pharmacol 1991; 42(1): 123-30.
[] [PMID: 1648919]
Tsukimi Y, Ushiro T, Yamazaki T, et al. Studies on the mechanism of action of the gastric H+,K(+)-ATPase inhibitor SPI-447. Jpn J Pharmacol 2000; 82(1): 21-8.
[] [PMID: 10874584]
Park S, Lee S, Song K, Lee B, Kang H, Kang J. The pharmacological properties of a novel acid pump antagonist, YH1885. Gut 2003; 52: A62.
Gedda K, Briving C, Svensson K, Maxvall I, Andersson K. Mechanism of action of AZD0865, a K+-competitive inhibitor of gastric H+, K+-ATPase. Biochem Pharmacol 2007; 73(2): 198-205.
[] [PMID: 17081503]
Hori Y, Imanishi A, Matsukawa J, et al. 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 2010; 335(1): 231-8.
[] [PMID: 20624992]
Sugano K, Sugano K. Vonoprazan fumarate, a novel potassiumcompetitive acid blocker, in the management of gastroesophageal reflux disease: Safety and clinical evidence to date. Therap Adv Gastroenterol 2018; 11: 1756283X17745776.
Kahrilas PJ, Dent J, Lauritsen K, et al. A randomized, comparative study of three doses of AZD0865 and esomeprazole for healing of reflux esophagitis. Clin Gastroenterol Hepatol 2007; 5(12): 1385-91.
[] [PMID: 17950677]
Dent J, Kahrilas PJ, Hatlebakk J, et al. 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 2008; 103(1): 20-6.
[] [PMID: 18184117]
Lee KJ, Son BK, Kim GH, et al. Randomised phase 3 trial: Tegoprazan, a novel potassium-competitive acid blocker, vs. esomeprazole in patients with erosive oesophagitis. Aliment Pharmacol Ther 2019; 49(7): 864-72.
[] [PMID: 30843245]
Oh J, Lee S, Moon SJ, Lee SC, Lee A, Jang IJ. Pharmacokinetics, pharmacodynamics and tolerability of DWP14012, a novel acid pump antagonist, in healthy subjects. Gastroenterology 2017; 152(5): S464.
Li C, Su M, Yan Y, et al. KFP-H008 blocks gastric acid secretion through inhibiting H+-K+-ATPase. Eur J Pharmacol 2017; 810: 112-9.
[] [PMID: 28629736]
Hwang JG, Yoo H, Lee JW, Song GS, Lee S, Kim MG. Comparison of pharmacokinetic characteristics of two Tegoprazan (CJ-12420) formulations in healthy male subjects. Transl Clin Pharmacol 2019; 27(2): 80-5.
[] [PMID: 32055586]
Han S, Choi HY, Kim YH, et al. Randomised clinical trial: Safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple oral doses of tegoprazan (CJ-12420), a novel potassium-competitive acid blocker, in healthy male subjects. Aliment Pharmacol Ther 2019; 50(7): 751-9.
[] [PMID: 31437865]
He J, Cao G, Yu J, et al. Safety, tolerability and pharmacokinetics of single ascending and multiple oral doses of tegoprazan in healthy chinese subjects. Clin Drug Investig 2021; 41(1): 89-97.
[] [PMID: 33355910]
Yoon DY, Sunwoo J, Shin N, et al. Effect of meal timing on pharmacokinetics and pharmacodynamics of tegoprazan in healthy male volunteers. Clin Transl Sci 2021; 14(3): 934-41.
[] [PMID: 33382926]
Han S, Choi HY, Kim YH, et al. Effect of food on the pharmacokinetics and pharmacodynamics of a single oral dose of tegoprazan. Clin Ther 2021; 43(8): 1371-80.
[] [PMID: 34246485]
Kim SH, Cho KB, Chun HJ, et al. Randomised clinical trial: Comparison of tegoprazan and placebo in non‐erosive reflux disease. Aliment Pharmacol Ther 2021; 54(4): 402-11.
[] [PMID: 34227708]
Howard PJ, Heading RC. Epidemiology of gastro-esophageal reflux disease. World J Surg 1992; 16(2): 288-93.
[] [PMID: 1561813]
Clarrett DM, Hachem C. Gastroesophageal Reflux Disease (GERD). Mo Med 2018; 115(3): 214-8.
[PMID: 30228725]
Scarpignato C, Hunt R. Proton pump inhibitors: The beginning of the end or the end of the beginning? Curr Opin Pharmacol 2008; 8(6): 677-84.
[] [PMID: 18840545]
Chen CL, Hsu PI. Current advances in the diagnosis and treatment of nonerosive reflux disease. Gastroenterol Res Pract 2013; 2013: 1-8.
[] [PMID: 23935610]
El-Serag HB. Epidemiology of non-erosive reflux disease. Digestion 2008; 78(S1): 6-10.
[] [PMID: 18832834]
Warren JR, Marshall B. Unidentified curved bacilli on gastric epithelium in active chronic gastritis. Lancet 1983; 1(8336): 1273-5.
[PMID: 6134060]
Malfertheiner P. Bismuth improves PPI-based triple therapy for H. pylori eradication. Nat Rev Gastroenterol Hepatol 2010; 7(10): 538-9.
[] [PMID: 20890314]
Nabeta H, Shinozaki S, Abe Y, et al. A potassium-competitive acid blocker-based regimen as second-line therapy improves Helicobacter pylori eradication. Digestion 2020; 101(3): 332-8.
[] [PMID: 30991394]
Lee JW, Kim N, Nam RH, et al. Efficacy of tegoprazan for improving the susceptibility of antimicrobial agents against antibiotic-resistant Helicobacter pylori. Gut Liver 2021; 15(1): 53-60.
[] [PMID: 33191308]

Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy