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Novel Therapy Shows Potential for Acid Suppression
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Tegoprazan, a novel therapy for GERD, was well-tolerated and showed rapid, dose-dependent acid suppression, according to results of a phase 1 study.
Kyun-Seop Bae, MD, PhD, of the department of clinical pharmacology and therapeutics at the University of Ulsan in South Korea, and colleagues wrote that tegoprazan (CJ HealthCare), is a potassium-competitive acid blocker (P-CAB) that works by reversibly suppressing gastric H+/K+ATPase.
“P-CABs bind to both the active and inactive forms of the ATPase,” they wrote. “P-CAB-induced gastric acid suppression is expected to be unaffected by the de novo synthesis of the proton pumps within gastric parietal cells, enabling a more rapid onset of maximum suppression and longer duration of action if appropriate pharmacokinetics are achieved.”
Researchers conducted a phase 1, randomized, double blind and placebo-controlled trial comprising 56 healthy men without Helicobacter pylori infection. In a single ascending dose study, they randomly assigned 32 men to receive 50, 100, 200 and 400 mg of tegoprazan or placebo. In a multiple ascending dose study, 16 individuals received 100 and 200 mg of tegoprazan or placebo every 24 hours. Researchers also performed a comparative pharmacodynamics study in which eight individuals received 40 mg of esomeprazole once a day for a week.
The analysis included safety, tolerability, pharmacodynamics (assessed through 24-hour gastric pH monitoring) and pharmacokinetics of the drug in plasma and urine.
Investigators found that tegoprazan was generally well-tolerated, and most adverse events were mild and easily resolved.
Exposure to the drug increased in a dose-proportional manner, and multiple dosing showed no accumulation in plasma after one week.
After single doses of 50, 100, 200 and 400 mg of tegoprazan, the gastric pH rose substantially and quickly at all dose levels. Investigators noted that these findings indicate that tegoprazan showed rapid onset of action with dose-dependency in the dose range. They had similar findings in the 100 and 200 mg multiple daily administration groups.
In the comparative pharmacodynamics study, researchers found that gastric Ph rose slowly compared with results in the tegoprazan studies. While esomeprazole induced the maximum pH level in 4 to 5 hours, 100 and 200 mg of tegoprazan reached that level in 1 hour.
“Throughout the study, tegoprazan appeared to be safe and well-tolerated at single doses of up to 400 mg and multiple doses up to 200 mg,” Bae and colleagues wrote. “The tolerable dose ranges, [pharmacokinetics] and [pharmacodynamics] characteristics of tegoprazan evaluated in this study will be useful in the further clinical development of tegoprazan.” – by Alex Young
Disclosures: Bae reports no relevant financial disclosures. Please see the full study for all other authors’ relevant financial disclosures.
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