Beiwen Keverprazan Hydrochloride Tablets

1. Indications and Usage
Reflux Esophagitis (RE): Treatment of adult patients with reflux esophagitis (up to 8 weeks).
Duodenal Ulcer (DU): Treatment of adult patients with duodenal ulcer (up to 6 weeks).
2. Dosage and Administration
Route of Administration: Oral administration ONLY.
Recommended Dosage: 20 mg once daily.
Critical Administration Instructions:
Timing: Preferably administered before breakfast.
Swallowing: Tablets must be swallowed whole; do not chew, crush, or break.
Duration: Data does not support use beyond 8 weeks for RE or 6 weeks for DU.
3. Mechanism of Action
K+-Competitive Acid Blockade: Keverprazan reversibly and competitively binds to the K+ binding site of the gastric H+/K+-ATPase (proton pump).
Inhibition of Acid Secretion: By blocking K+ ions from binding to the enzyme, it inhibits both basal and stimulated gastric acid secretion.
Pharmacokinetic Advantage: Unlike traditional proton pump inhibitors (PPIs), it provides rapid onset and stable acid suppression without requiring acidic activation, and its effect is not significantly influenced by food intake.
4. Safety and Warnings
Hepatotoxicity: Liver function abnormalities (elevated ALT/AST) have been reported. Monitoring is recommended, and the drug should be discontinued if signs of liver insufficiency appear.
Contraindications: Contraindicated in patients with known hypersensitivity. It is contraindicated in patients taking atazanavir, nelfinavir, or rilpivirine due to pharmacokinetic interactions.
Masking Malignancy: May mask symptoms of gastric malignancy; malignancy should be ruled out before initiating therapy.
Infection Risk: Increased gastric pH may increase the risk of gastrointestinal infections (e.g., Salmonella, Campylobacter, C. difficile).
Fracture Risk: Long-term use (≥1 year) at high doses may increase the risk of osteoporosis-related fractures.
Hypomagnesemia: Rare cases of symptomatic hypomagnesemia have been reported with ≥3 months of treatment.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions: Diarrhea, constipation, abdominal pain, nausea, and taste disturbance (dysgeusia).
Laboratory Abnormalities: Increases in ALT, AST, uric acid, and triglycerides; decreases in neutrophil counts.
Clinical Research Highlights: Phase 3 trials demonstrated that 20 mg once daily was effective and well-tolerated in healing esophagitis and duodenal ulcers.
6. Drug Interactions
CYP3A4 Inhibitors/Inducers: As a substrate of CYP3A4, concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole) or inducers (e.g., rifampicin) requires clinical caution.
Acid-Dependent Drugs: Due to increased gastric pH, absorption of drugs dependent on gastric acidity (e.g., atazanavir, nelfinavir, rilpivirine, iron salts, ketoconazole) may be significantly reduced.
7. Pharmaceutical Information
Chemical Composition: Active Ingredient: Keverprazan Hydrochloride.
Appearance: Film-coated tablets, white or off-white.
Packaging: Blister packaging (e.g., 10 mg or 20 mg per tablet).
Storage: Store at controlled room temperature; protect from moisture.