Pharmacokinetic and Pharmacodynamic Characteristics of Tegoprazan According to Helicobacter pylori Infection Status.

OBJECTIVE: Tegoprazan is a novel potassium-competitive acid blocker (P-CAB) used to treat acid-related diseases. This study aimed to evaluate the effect of the H. pylori infection status on the pharmacokinetic (PK) and pharmacodynamic (PD) characteristics and safety of tegoprazan. METHODS: This study involved two cohorts. In Cohort 1, 12 H. pylori-negative subjects were administered tegoprazan at 50 or 100 mg for 7 days. In Cohort 2, four subjects positive for H. pylori received 50 and 100 mg of tegoprazan in a single dose crossover study. We estimated the PK parameters using non-compartment analysis and measured PD parameters using an intragastric pH monitor. RESULTS: The PK and PD of tegoprazan in both groups were dose-dependent. The Cmax of each dose of tegoprazan in subjects with H. pylori decreased more than in the H. pylori negative group, but the AUClast and AUCinf of the two groups were similar. All PD parameters in H. pylori-positive subjects increased more than in the negative group, which suggests that tegoprazan's intragastric acid suppression is enhanced in cases of H. pylori. CONCLUSION: The presence of H. pylori did not have a clinically significant effect on tegoprazan's PK and tolerability, but significantly enhanced its intragastric acid suppression efficacy.