Transl Clin Pharmacol.  2019 Jun;27(2):80-85. 10.12793/tcp.2019.27.2.80.

Comparison of pharmacokinetic characteristics of two Tegoprazan (CJ-12420) formulations in healthy male subjects

• Hwang JG
• Yoo H
• Lee JW
• Song GS
• Lee S
• Kim MG

• KMID: 2457576
• DOI: http://doi.org/10.12793/tcp.2019.27.2.80

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.

Keyword

Bioequivalence; Clinical trial; Pharmacokinetics; Phase 1

MeSH Terms

Gastroesophageal Reflux
Healthy Volunteers
Humans
Male*
Mass Spectrometry
Methods
Pharmacokinetics
Plasma
Tablets
Therapeutic Equivalency
Tablets

Figure

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  Figure 1 Study design. (Reference drug = tegoprazan formulation 1, Test drug = tegoprazan formulation 2). Six subjects were allocated to each sequence group.

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  Figure 2 Mean plasma tegoprazan concentration-time profiles after a single oral dose of test or reference formulation of 100 mg tegoprazan tablet (left: linear scale, right: semi-log scale).

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  Figure 3 Mean plasma M1 concentration-time profiles after a single oral dose of test or reference formulation of 100 mg tegoprazan tablet (left: linear scale, right: semi-log scale).

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