Effect of meal timing on pharmacokinetics and pharmacodynamics of
tegoprazan in healthy male volunteers
Abstract
Tegoprazan, a novel potassium-competitive acid blocker, is used to treat
acid-related diseases. However, there is no information on the
pharmacokinetic (PK) and pharmacodynamic (PD) profiles of the marketed
dosage of tegoprazan under various meal timings in a fed and fasted
state. The study aimed to assess the effect of meal timing on PKs and
PDs of tegoprazan 50 mg after a single administration in healthy male
subjects. An open-label, single-dose, three-treatment, three-period
crossover study was conducted. A total of 12 subjects were orally
administered a single dose of tegoprazan 50 mg among various conditions:
in a fasted state, at 30 min before or 30 min after a high-fat meal. PK
parameters were estimated by non-compartmental method. Continuous
24-hour intragastric pH monitoring was done for PD analysis. The PKs and
PDs of tegoprazan were compared among the various meal timings. Compared
to the fasting condition, the PK profile of tegoprazan was similar when
administered 30 min before a high-fat meal; however, delayed absorption
with similar systemic exposure was observed when administered 30 min
after a high-fat meal. The magnitude of acid suppression evaluated
through the PD parameters increased when administered 30 min after a
high-fat meal compared to fasting the condition and when administered 30
min before a high-fat meal. However, the increased difference in acid
suppression was not clinically significant. Meal timing had no
clinically significant effect on the PKs and PDs of tegoprazan 50 mg.
Therefore, the marketed dosage of tegoprazan could be administered
regardless of the meal timing.