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Randomized Controlled Trial
. 2022 Jul;88(7):3288-3296.
doi: 10.1111/bcp.15268. Epub 2022 Feb 23.

Night-time gastric acid suppression by tegoprazan compared to vonoprazan or esomeprazole

Eunsol Yang  1 , Seokuee Kim  2 , Bongtae Kim  2 , Boram Kim  3 , Yechan Kim  3 , Sung Sup Park  3 , Geun Seog Song  2 , Kyung-Sang Yu  1 , In-Jin Jang  1 , SeungHwan Lee  1
Affiliations
Randomized Controlled Trial

Night-time gastric acid suppression by tegoprazan compared to vonoprazan or esomeprazole

Eunsol Yang et al. Br J Clin Pharmacol. 2022 Jul.

Abstract

Aims: Nocturnal acid breakthrough has been considered an unmet need of proton-pump inhibitors. Tegoprazan, a novel potassium-competitive acid blocker, is expected to show improved properties for this unmet need. This study was aimed to compare night-time acid suppression by tegoprazan with that by vonoprazan or esomeprazole, and to explore the effect of CYP2C19 phenotypes on acid-suppressive effects.

Methods: A randomized, open-label, 3-period, 6-sequence crossover study was conducted. A single oral dose of tegoprazan 50 mg, vonoprazan 20 mg or esomeprazole 40 mg was administered at night in each period. Continuous intragastric pH was monitored at baseline and after each dosing.

Results: Sixteen healthy subjects (6 CYP2C19 extensive metabolizers, 5 intermediate metabolizers, 5 poor metabolizers) completed the study. After a single dose of tegoprazan, intragastric pH increased more rapidly to over 4 at approximately 1 hour compared to the other treatments, and elevated intragastric pH was maintained stably at night. Tegoprazan exhibited night-time acid suppression for slightly but not significantly longer than vonoprazan, and greater than esomeprazole; % time at pH ≥ 4 at night was 66.0%, 60.5% and 36.1% for tegoprazan, vonoprazan and esomeprazole, respectively. Night-time acid suppression by tegoprazan and vonoprazan was not dependent on CYP2C19 phenotypes, while that by esomeprazole tended to be influenced by CYP2C19 phenotypes.

Conclusion: Tegoprazan produced more rapid, potent and well sustained night-time acid suppression vs. vonoprazan or esomeprazole when administered at night. Furthermore, tegoprazan showed no CYP2C19 phenotype dependency in acid suppression. It suggests the potential of tegoprazan, especially in preventing nocturnal acid breakthrough.

Keywords: CYP2C19 genetic polymorphisms; gastroesophageal reflux disease; nocturnal acid breakthrough; potassium-competitive acid blocker; proton-pump inhibitor.

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Conflict of interest statement

Seokuee Kim, Bongtae Kim and Geun Seog Song are employees of HK inno. N Corp. The other authors report no conflicts of interest in this work.

Figures

FIGURE 1
FIGURE 1
Study design. Night was defined as the period of 12 hours from 22:00 to 10:00 hours
FIGURE 2
FIGURE 2
Mean night‐time intragastric pH–time profiles at baseline (predose) and after a single oral administration of tegoprazan 50 mg, vonoprazan 20 mg or esomeprazole 40 mg under fasted condition. The background shadow represents standard deviation. Night was defined as the period of 12 hours from 22:00 to 10:00 hours
FIGURE 3
FIGURE 3
Mean night‐time percentage of time that the intragastric pH was over 4 (% time at pH ≥ 4) for (A) each treatment in all CYP2C19 phenotypes, and for (B) tegoprazan 50 mg, (C) vonoprazan 20 mg and (D) esomeprazole 40 mg according to CYP2C19 phenotypes. Night was defined as the period of 12 hours from 22:00 to 10:00 hours
FIGURE 4
FIGURE 4
Point estimates and 95% confidence intervals of the mean differences between CYP2C19 phenotypes for night (A) percentage of time that the intragastric pH was >4 (% time at pH ≥ 4), (B) median pH and (C) mean pH after a single oral administration of tegoprazan 50 mg, vonoprazan 20 mg or esomeprazole 40 mg under fasted condition. Night was defined as the period of 12 hours from 22:00 to 10:00 hours
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References

    1. Kellerman R, Kintanar T. Gastroesophageal Reflux Disease. Prim Care. 2017;44(4):561‐573. doi:10.1016/j.pop.2017.07.001 - DOI - PubMed
    1. Chen J, Brady P. Gastroesophageal Reflux Disease: Pathophysiology, Diagnosis, and Treatment. Gastroenterol Nurs. 2019;42(1):20‐28. doi:10.1097/sga.0000000000000359 - DOI - PubMed
    1. Bell NJ, Burget D, Howden CW, Wilkinson J, Hunt RH. Appropriate acid suppression for the management of gastro‐oesophageal reflux disease. Digestion. 1992;51(Suppl 1):59‐67. doi:10.1159/000200917 - DOI - PubMed
    1. Peghini PL, Katz PO, Bracy NA, Castell DO. Nocturnal recovery of gastric acid secretion with twice‐daily dosing of proton pump inhibitors. Am J Gastroenterol. 1998;93(5):763‐767. doi:10.1111/j.1572-0241.1998.221_a.x - DOI - PubMed
    1. Tutuian R, Castell DO. Nocturnal acid breakthrough ‐ approach to management. MedGenMed. 2004;6(4):11‐11. - PMC - PubMed

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