Tenatoprazole, a novel proton pump inhibitor with a prolonged plasma half-life: effects on intragastric pH and comparison with esomeprazole in healthy volunteers

Abstract

Background: Proton pump inhibitors control gastric acidity better during the day than at night, when nocturnal acid breakthrough can occur. Tenatoprazole is a novel proton pump inhibitor with a seven-fold longer plasma half-life. Aim : To compare the effects of tenatoprazole 20 mg (T20), tenatoprazole 40 mg (T40) and esomeprazole 40 mg (E40) on intragastric acidity in healthy volunteers.

Methods: This randomized, three-period, cross-over study enrolled 18 Helicobacter pylori-negative volunteers, who received E40, T20 and T40 once daily for 7 days with a 14-day washout between periods. Twenty-four-hour gastric pH monitoring was performed on day 7. Serum gastrin was assessed on day 8.

Results: T40 induced a more potent acid inhibition than T20 (24-h median pH: 4.6 vs. 4.0, P < 0.01; daytime: 4.5 vs. 3.9, P < 0.01; night-time: 4.7 vs. 4.1, P < 0.05). T40 was more potent than E40 (24-h median pH: 4.6 vs. 4.2, P < 0.05; night-time: 4.7 vs. 3.6, P < 0.01); the pH > 4 holding time was higher during the night for T40 than for E40: 64.3% vs. 46.8%, P < 0.01; the nocturnal acid breakthrough duration was significantly shorter for T40 than for E40. No significant gastrin increase was observed and all drugs were well tolerated.

Conclusion: T40 is significantly more potent than T20 and E40 during the night. The therapeutic relevance of this pharmacological advantage deserves further study.