A randomized, open-label, single-dose study to evaluate the safety and pharmacokinetics of two formulations containing 40 mg of fexuprazan in healthy Korean subjects.

Abstract

Objective: To evaluate the pharmacokinetics and safety of two 40-mg fexuprazan formulations.

Materials and methods: This study was an open-label, randomized, single-dose, crossover bioequivalence trial in healthy subjects. 24 subjects were randomized to receive either the test formulation, tablet A (40 mg fexuprazan), or the reference formulation, tablet B (40 mg fexuprazan), with crossover administration. Plasma samples were collected up to 48 hours post-dose and analysed for fexuprazan using a validated liquid chromatography-tandem mass spectrometry (LC-MS/MS). Individual pharmacokinetic parameters were derived by noncompartmental analysis. Safety was evaluated throughout the study.

Results: 22 subjects completed the study and were included in the pharmacokinetic analysis. Geometric mean values of area under the plasma concentration-time curve from time zero to the last quantifiable concentration (AUC_t) was 380.17 and 390.33 ng×h/mL for the test and reference formulations, respectively. Geometric mean values of maximum plasma concentration (C_max) were 29.36 and 31.65 ng/mL for the test and reference formulations, respectively. The 90% confidence intervals (CIs) for the test/reference geometric mean ratios of AUC_t and C_max were 0.9098 - 1.0427 and 0.8665 - 0.9931, respectively. All adverse events were mild, and no serious adverse events occurred.

Conclusion: The novel 40-mg fexuprazan formulation (tablet A) was demonstrated to be bioequivalent to the initially developed formulation (tablet B), with comparable systemic exposure (AUC) and peak concentration (C_max). Both formulations were well tolerated, with no clinically meaningful differences in adverse event profiles.