Vonoprazan is a potassium competitive acid blocker used in the treatment of acid related diseases and as an adjuvant drug for eradicating Helicobacter pylori.
Vonoprazan is a potassium competitive acid blocker (PCAB) that can inhibit H+, K+- atpase mediated gastric acid secretion. PCab represents an alternative solution for proton pump inhibitors in the treatment of acid related diseases. Different from proton pump inhibitor, pcab is not affected by CYP2C19 gene polymorphism, and does not need acid resistant formula. In addition, vonoprazan is 350 times more effective than the proton pump inhibitor lansoprazole, because vonoprazan can accumulate in the main gastric mucosa, especially in gastric parietal cells.
In February 2015, vonoprazan was first launched in Japan as an adjuvant therapy for treating acid-related diseases and eradicating Helicobacter pylori (H. pylori). In May 2022, the FDA approved the use of vonoprazan in co packaged products containing amoxicillin and clarithromycin for the treatment of Helicobacter pylori infection. Studies have shown that the simultaneous use of vonoprazine, amoxicillin, and clarithromycin can achieve a Helicobacter pylori eradication rate of approximately 90%.
Vonoprazan is packaged in combination with amoxicillin and clarithromycin for the treatment of adult Helicobacter pylori (H. pylori) infection. Another co packaged product that only contains vornoprazan and amoxicillin is also suitable for treating adult Helicobacter pylori infections.
The use of vornoprazan leads to an increase in gastric pH. The inhibitory effect of vornoprazan on gastric acid secretion increases with repeated daily administration. Although the anti secretory effect of vornoprazine weakened after discontinuation, the gastric pH remained elevated for 24-48 hours. Vonoprazan has no significant clinical impact on QT interval prolongation.
Compared with other potassium competitive acid blockers (pcab), vonoprazan has a higher point positive charge (pKa 9.06). This allows vonoprazan to accumulate at a higher concentration in the lumen of gastric parietal cells, where it binds H+, K+- atpase in a K+competitive and reversible manner. Compared with other PCABs (such as SCH28080) or proton pump inhibitors (such as Lansoprazole), vonoprazan has more effective H+, K+- atpase inhibitory activity.