Mass balance and metabolite profiles in humans of tegoprazan, a novel potassium-competitive acid blocker, using 14C-radiolabelled techniques
Abstract
ABSTRACT Background Tegoprazan (LXI-15028), a novel potassium-competitive acid blocker, has shown great efficacy in treating acid-related disorders. However, its metabolic and excretion characteristics are not fully understood. Research design and methods A single oral dose of 50 mg/150 μCi [14C]tegoprazan was administered to six healthy subjects. Blood, urine and fecal samples were collected and measured for total radioactivity (TRA), tegoprazan and metabolites. Its safety was also assessed. Results The maximum concentrations (Cmax) of tegoprazan and TRA in plasma were 634 ng/mL and 990 ng eq./mL, respectively, at 0.5 h post dose. Tegoprazan and its N-demethylation metabolite (M1) were the major drug-related compounds in plasma, accounting for 34.84% and 40.10% of TRA, respectively. The half-life (t1/2) of TRA (8.72 h) was longer than that of tegoprazan (4.33 h) in plasma, indicating slower metabolite elimination. Tegoprazan was excreted through both the urine (50.51 ± 3.35%) and feces (47.26 ± 3.06%). The main metabolic pathways of tegoprazan are demethylation, oxidation, glucuronidation and sulfation. There were no serious adverse events observed in this study. Conclusions Tegoprazan is widely metabolized and excreted completely in humans. Tegoprazan and M1 were the primary compounds present in the circulation. Clinical trial registration www.clinicaltrials.gov identifier is NCT05883306.
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Evidence Hub reads this as a clinical trial, done in people. Its evidence level is 3 of 5 (Moderate · trial / cohort / secondary analysis). Trials without a large randomized design, cohorts and secondary analyses give moderate evidence.
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