Comparison of pharmacokinetic characteristics of two Tegoprazan (CJ-12420) formulations in healthy male subjects
10.12793/tcp.2019.27.2.80
- Author:
Jun Gi HWANG
1
;
Hyounggyoon YOO
;
Ji Won LEE
;
Geun Seog SONG
;
SeungHwan LEE
;
Min Gul KIM
Author Information
1. Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital, Seoul 03080, Republic of Korea.
- Publication Type:Clinical Trial
- Keywords:
Bioequivalence;
Clinical trial;
Pharmacokinetics;
Phase 1
- MeSH:
Gastroesophageal Reflux;
Healthy Volunteers;
Humans;
Male;
Mass Spectrometry;
Methods;
Pharmacokinetics;
Plasma;
Tablets;
Therapeutic Equivalency
- From:Translational and Clinical Pharmacology
2019;27(2):80-85
- CountryRepublic of Korea
- Language:English
-
Abstract:
Proton-pump inhibitors (PPIs) are effectively used to treat acid-related diseases, including gastroesophageal reflux disease (GERD); however, many unmet medical needs still exist. As a new treatment option, potassium-competitive acid blockers (P-CABs), such as tegoprazan, have been developed. This study was performed to compare the pharmacokinetics (PKs) between two formulations (test and reference drugs) of tegoprazan 100 mg tablets. A randomized, single oral dose, two-treatment, two-period, two-sequence study was conducted with 12 healthy subjects. Each subject received the test drug or reference drug in the first period and the alternative treatment in the second period. For PK evaluation, blood samples were collected up to 48 hours post-dose in each period. The plasma concentrations of tegoprazan and its active metabolite (M1) were measured by liquid chromatography-tandem mass spectrometry. PK parameters, including maximum plasma concentration (C(max)) and area under the concentration-time curve from zero to the last measurable time (AUC(last)), were estimated using a non-compartmental method. The plasma concentration-time profiles of the two formulations were comparable. The geometric mean ratios [90% confidence intervals (CIs)] of the test drug to the reference drug for C(max) and AUC(last) were 0.98 (0.85–1.12) and 1.03 (0.93–1.13), respectively. The corresponding values of M1 were 0.99 (0.89–1.11) and 1.01 (0.93–1.09), respectively. The two formulations of tegoprazan exhibited comparable PK profiles, fulfilling the regulatory criteria for bioequivalence.
