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Research ArticleDrug Discovery and Translational Medicine

Tegoprazan, a Novel Potassium-Competitive Acid Blocker to Control Gastric Acid Secretion and Motility

Nobuyuki Takahashi and Yukinori Take
Journal of Pharmacology and Experimental Therapeutics November 27, 2017, jpet.117.244202; DOI: https://doi.org/10.1124/jpet.117.244202
Nobuyuki Takahashi
1 RaQualia Pharma Inc;
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Yukinori Take
2 RaQualia Pharma Inc.
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Abstract

Tegoprazan, (S)-4-((5,7-difluorochroman-4-yl)oxy)-N,N,2-trimethyl-1H-benzo[d]imidazole-6-carboxamide, a potassium-competitive acid blocker (P-CAB), is a novel potent and highly selective inhibitor of gastric H+/K+-ATPase. Tegoprazan inhibited porcine, canine, and human H+/K+-ATPases in vitro with IC50 values ranging 0.29 ~ 0.52 μM while that for canine kidney Na+/K+-ATPase was more than 100 μM. A kinetic analysis revealed that tegoprazan inhibited H+/K+-ATPase with potassium-competitive manner and the binding was reversible. Oral single administrations of tegoprazan ranging 0.3 ~ 30 mg/kg in dogs were well absorbed into blood stream and distributed in gastric tissue/fluid higher than in plasma. Tegoprazan potently inhibited histamine-induced gastric acid secretion in dogs and a complete inhibition was observed at 1.0 mg/kg starting from 1 hr after administration. Moreover, an oral administration of tegoprazan at 1 and 3 mg/kg reversed the pentagastrin-induced acidified gastric pH to the neutral range. Interestingly, 3 mg/kg tegoprazan immediately evoked a gastric phase III contraction of migrating motor complex (MMC) in pentagastrin-treated dogs and similar effects was observed with the other P-CAB, vonoprazan.  Tegoprazan is the novel P-CAB which may provide a new option for the therapy of gastric acid-related and motility-impaired diseases.

  • acid secretion
  • gastric ulcer
  • gastrointestinal motility
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 377 (2)
Journal of Pharmacology and Experimental Therapeutics
Vol. 377, Issue 2
1 May 2021
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Research ArticleDrug Discovery and Translational Medicine

Tegoprazan, a Novel Potassium-Competitive Acid Blocker to Control Gastric Acid Secretion and Motility

Nobuyuki Takahashi and Yukinori Take
Journal of Pharmacology and Experimental Therapeutics November 27, 2017, jpet.117.244202; DOI: https://doi.org/10.1124/jpet.117.244202

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Research ArticleDrug Discovery and Translational Medicine

Tegoprazan, a Novel Potassium-Competitive Acid Blocker to Control Gastric Acid Secretion and Motility

Nobuyuki Takahashi and Yukinori Take
Journal of Pharmacology and Experimental Therapeutics November 27, 2017, jpet.117.244202; DOI: https://doi.org/10.1124/jpet.117.244202
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