Pharmacodynamics of tegoprazan and revaprazan after single and multiple oral doses in healthy subjects

Abstract

SummaryBackgroundPotassium‐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.AimsTo evaluate the pharmacodynamics and safety/tolerability of tegoprazan and revaprazan after single and multiple oral dosesMethodsA 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.ResultsAfter 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.ConclusionTegoprazan 50 mg showed stronger gastric acid suppression than revaorazan 200 mg. Both drugs were well tolerated.

Efficacy and safety of tegoprazan in the treatment of gastroesophageal reflux disease: A protocol for meta-analysis and systematic review

“…This study showed that tegoprazan 50 and 100 mg showed better results compared to placebo for NERD. All three clinical trials [30][31][32] reported treatment emergent adverse events (TEAEs), most of which were mild and tolerated by patients. The more common TEAEs for tegoprazan were mainly gastrointestinal adverse events (2% ~4.9%) and headache (1% ~4.9%), with no significant differences compared with positive controls or placebo.…”

Potassium-Competitive Acid Blockers for the Treatment of Gastroesophageal Reflux Disease

“…In Korean subjects, tegoprazan 50 mg once-daily and revaprazan 200 mg once-daily for 7 days maintained intragastric pH above 4 for 68.2% and 25.3%, respectively, of the 24-hour recording period. 31…”

Editorial: deja vu all over again – let the P‐CAB wars begin. Authors' reply

“…4 In contrast, other P-CABs such as tegoprazan and fexuprazan have shown comparable increases in serum gastrin levels to esomeprazole, despite their more potent inhibition of gastric acid secretion. [5][6][7][8] Tegoprazan increased serum gastrin level to about 200 pg/mL after administration of 200 mg once-daily for 1 week, while esomeprazole 40 mg increased serum gastrin to about 200 pg/mL. Similarly, fexuprazan increased serum gastrin level to about 200 and 150 pg/mL after administration of 40 mg once-daily for 1 and 8 weeks, respectively, while esomeprazole 40 mg increased serum gastrin to about 200 and 150 pg/mL, respectively.…”