Pharmacodynamics Between a Dual Delayed-Release Formulation of Low-Dose Esomeprazole and Famotidine in Healthy Korean Subjects

• Published in: Clinical therapeutics Vol. 46; no. 8; pp. 622 - 628
• Main Authors: Choi, Young-Sim, Hwang, Jun Gi, Kim, Jae-Won, Min, Hyojin, Seong, Chang-Hwan, Hong, Sung Hee, Kim, Na Young, Park, Min Kyu
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.08.2024; Elsevier Limited
• Subjects: Acidity; Acids; Adult; Antacids; Anti-Ulcer Agents - administration & dosage; Anti-Ulcer Agents - pharmacokinetics; Anti-Ulcer Agents - pharmacology; Cross-Over Studies; Delayed-Action Preparations; Dosage; Drug delivery; Drug dosages; Dual delayed-release esomeprazole; Esomeprazole - administration & dosage; Esomeprazole - pharmacology; Famotidine; Famotidine - administration & dosage; Female; Gastric Acid - metabolism; Gastric Acidity Determination; Gastric mucosa; Gastritis; Gastritis - drug therapy; Gastroesophageal reflux; Gastrointestinal diseases; Healthy Volunteers; Histamine; Histamine H2 receptors; Humans; Hydrogen-Ion Concentration; Internal Medicine; Male; Omeprazole; Peptic ulcers; pH effects; Pharmacodynamics; Pharmacokinetics; Proton pump inhibitors; Proton Pump Inhibitors - administration & dosage; Proton Pump Inhibitors - pharmacology; Republic of Korea; Safety; Stomach; Young Adult; Republic of Korea; South Korea; Famotidine; Pharmacodynamics; Safety; Dual delayed-release esomeprazole; Pharmacokinetics; Gastritis
• ISSN: 0149-2918; 1879-114X; 1879-114X
• DOI: 10.1016/j.clinthera.2024.06.013

Gastritis, one of the most common clinically diagnosed conditions, is defined as the infiltration of inflammatory cells into the gastric mucosa. Drugs for gastritis include histamine-2 receptor antagonists and proton pump inhibitors (PPIs), which reduce acidity in the stomach, and antacids, which neutralize acid. Esomeprazole is a PPI for gastroesophageal reflux disease and gastric and duodenal ulcers that has been shown to be safe and effective at a 10 mg dose. Dual-release drugs have not yet been approved for the treatment of gastritis domestically or internationally. In this study, a dual delayed-release (DR) esomeprazole (10 mg), was compared to famotidine (20 mg) to determine its effectiveness in the treatment of gastritis. This study was a randomized, open-label, multiple-dose, 2-treatment, 2-period, 2-sequence crossover study with a 7-day washout between periods. In each period, the subjects were administered one dose of esomeprazole (10 mg) or famotidine (20 mg) for 7 days at each period. The 24-hour gastric pH was recorded after single and multiple doses. The percentage of time (duration%) that the pH was maintained above 4 in the 24 hours after 7 days of repeated dosing was evaluated. The mean percentages of time that the gastric pH was above 4 after multiple doses over 7 days of a dual DR esomeprazole (10 mg) and famotidine (20 mg) was 47.31% ± 14.85% and 23.88% ± 10.73%. Multiple doses of a dual DR esomeprazole (10 mg) showed effective gastric acid secretion suppression compared to famotidine with comparable safety and tolerability. These results provide evidence supporting the clinical use of a dual DR esomeprazole (10 mg) to treat gastritis. ClinicalTrials.gov identifier: NCT04967014.