Effect of Food on the Pharmacokinetics, Pharmacodynamics, and Safety of Zastaprazan, a Potassium-Competitive Acid Blocker, in Healthy Participants.
Hyoeun Lee, Seok-Kyu Yoon, Soo-Min Jung et al.
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In 30 seconds
This randomized, open-label, two-period crossover phase 1 study assessed food effects on zastaprazan pharmacokinetics, pharmacodynamics, and safety in 24 healthy participants given a single 20 mg dose. With food, peak exposure decreased (Cmax GMR, 0.6997; 90% CI, 0.6292-0.7781), while AUC last increased (GMR, 1.3783; 90% CI, 1.2688-1.4973) and Tmax was delayed. Despite these pharmacokinetic changes, acid suppression was comparable: intragastric pH ≥ 4 over 24 h was 70.01% fed versus 69.19% fasted. Zastaprazan was well tolerated, with no clinically significant safety concerns identified.
Key findings
- Fed dosing reduced Cmax (GMR, 0.6997; 90% CI, 0.6292-0.7781) but increased AUC last (GMR, 1.3783; 90% CI, 1.2688-1.4973).
- Time with intragastric pH ≥ 4 over 24 h was similar with food and fasting: 70.01% vs. 69.19%.
- Zastaprazan was well tolerated, and no clinically significant safety concerns were identified.
Why it matters
Food changed the rate and extent of zastaprazan absorption, but the measured acid-suppression response remained comparable in this healthy-participant study. This distinction is clinically relevant because pharmacokinetic differences do not necessarily translate into altered pharmacodynamic effect; here, the findings support flexibility around meal timing while remaining limited to the conditions studied.
What to keep in mind
The phase 1 study involved 24 healthy participants and assessed a single 20 mg dose, so it does not establish food effects during repeated dosing or in patients.