Novel acid-suppressive agent shows therapeutic potential

The novel potassium-competitive acid blocker zastaprazan (JP-1366) appears to have a rapid and potent gastric acid-suppressive effect, with a single oral dose up to 60 mg and multiple oral doses up to 40 mg being safe and well tolerated, according to a study.

Single and multiple ascending doses of zastaprazan were tested in healthy Korean men in this randomized, open-label, placebo- and active-controlled trial.

Pharmacodynamics was assessed using intragastric pH and serum gastrin, while pharmacokinetics was evaluated using serial blood and urine samples collected from the participants. A pharmacogenomic evaluation was also performed to explore genetic variants, which can affect the pharmacodynamics and pharmacokinetics. Finally, safety and tolerability, including hepatotoxicity, were examined.

The gastric acid secretion-suppression effect of zastaprazan was greater at higher doses. Zastaprazan 20 and 40 mg doses were either comparable to or more favourable than esomeprazole 40 mg in terms of the percentage of time that gastric pH was over 4 (%Time pH >4; 85.19 percent and 91.84 percent vs 72.06 percent).

Zastaprazan was absorbed into the body within 2 hours and eliminated with a half-life of 6–10 hours. Pharmacogenomic analysis showed no genetic variant of drug metabolizing enzymes, including CYP2C19 or drug transporters, associated with the exposure of zastaprazan.

Safety and tolerability assessments indicated that zastaprazan was well tolerated.

The findings suggest that the drug has pharmacodynamic and pharmacokinetic profiles suitable for treating patients with acid-related diseases.