BACKGROUND:Potassium-competitive acid blockers (P-CABs) are emerging as novel treatments for acid-related disorders including gastroesophageal reflux disease. Tegoprazan and revaprazan are approved P-CABs in South Korea, but the pharmacodynamics and safety/tolerability of the two drugs have never been compared. AIMS: To evaluate the pharmacodynamics and safety/tolerability of tegoprazan and revaprazan after single and multiple oral doses METHODS: A randomised, open-label, active-controlled study was conducted in Helicobacter pylori-negative healthy Korean male subjects. Tegoprazan 50 mg or revaprazan 200 mg was administered orally, once daily for 7 days; 24-h intragastric pHmonitoring and serum gastrin were measured for pharmacodynamic evaluation. Safety parameters including serum microRNA-122 (miR-122) level were also collected. RESULTS: After a single dose, the %Time pH ≥4 for tegoprazan was greater than that for revaprazan (54.5% vs 25.1%). After multiple doses, the %Time pH ≥4 for tegoprazan was also greater than that for revaprazan (68.2% vs 25.3%). %Time pH ≥4 during 12 hours at nighttime for tegoprazan was greater than that for revaprazan (71.8% vs 31.9%). The changes in the serum gastrin were not clinically significant for either drug. Despite the slight increases of serum miR-122 for each drug, tegoprazan and revaprazan were well tolerated considering other safety parameters including AST and ALT levels. CONCLUSION:Tegoprazan 50 mg showed stronger gastric acid suppression than revaorazan 200 mg. Both drugs were well tolerated.
RCT Entities:
BACKGROUND:Potassium-competitive acid blockers (P-CABs) are emerging as novel treatments for acid-related disorders including gastroesophageal reflux disease. Tegoprazan and revaprazan are approved P-CABs in South Korea, but the pharmacodynamics and safety/tolerability of the two drugs have never been compared. AIMS: To evaluate the pharmacodynamics and safety/tolerability of tegoprazan and revaprazan after single and multiple oral doses METHODS: A randomised, open-label, active-controlled study was conducted in Helicobacter pylori-negative healthy Korean male subjects. Tegoprazan 50 mg or revaprazan 200 mg was administered orally, once daily for 7 days; 24-h intragastric pH monitoring and serum gastrin were measured for pharmacodynamic evaluation. Safety parameters including serum microRNA-122 (miR-122) level were also collected. RESULTS: After a single dose, the %Time pH ≥4 for tegoprazan was greater than that for revaprazan (54.5% vs 25.1%). After multiple doses, the %Time pH ≥4 for tegoprazan was also greater than that for revaprazan (68.2% vs 25.3%). %Time pH ≥4 during 12 hours at nighttime for tegoprazan was greater than that for revaprazan (71.8% vs 31.9%). The changes in the serum gastrin were not clinically significant for either drug. Despite the slight increases of serum miR-122 for each drug, tegoprazan and revaprazan were well tolerated considering other safety parameters including AST and ALT levels. CONCLUSION: Tegoprazan 50 mg showed stronger gastric acid suppression than revaorazan 200 mg. Both drugs were well tolerated.