Acid cam qt1/6/2023 ![]() ![]() Vonoprazan (Takecab) was released to the market in Japan in February 2015. It was found to have satisfactory effects and a good safety profile in clinical studies of gastric and duodenal ulcers, reflux esophagitis, NSAID-associated ulcers, and H. With these efforts, vonoprazan (TAK-438), a potassium-competitive acid blocker (P-CAB), was developed. To overcome the aforementioned unmet needs, alternative formulations of conventional PPIs and new H +, K +-ATPase inhibitors have been established. 12– 14 Finally, although it requires an acidic environment for activation, PPIs are unstable in acidic conditions, 15 so enteric coating is needed. 10, 11 Third, its effects at night are not satisfactory. 9 Second, the effects of PPIs are influenced by cytochrome P450 (CYP) 2C19 polymorphism. 5– 7 Reflux symptoms of GERD are not sufficiently relieved after the first dose of PPIs in two-thirds of patients because of its slow onset of the action, 8, 9 and one-half of patients still have symptoms even after 3 days of treatment. 4 First, it takes several days to show maximal effect. 1– 3 Although PPIs have been used for more than a quarter-century as a first-line treatment for these diseases, it has become clear that there are some issues in need of improvement ( Table 1). Conventional PPIs with a benzimidazole structure irreversibly inhibit hydrogen potassium (H +, K +)-ATPases, which produce acid in gastric parietal cells and more strongly block acid secretion compared to histamine H2 receptor antagonists. Proton pump inhibitors (PPIs) have often been used for acid-related diseases including gastroesophageal reflux disease (GERD), gastric and duodenal ulcers, non-steroidal anti-inflammatory drug (NSAID)-associated ulcers, and Helicobacter pylori eradication therapy. Keywords: Anti-inflammatory agents, non-steroidal, Esophagitis, H +, K +-exchanging ATPase, Helicobacter pylori, Potassium-competitive acid blocker Thus, vonoprazan may address the unmet medical need for the treatment of acid-related diseases. It does not require an acidic environment for activation, has long-term stability at the site of action, and has satisfactory safety and tolerability. Vonoprazan accumulates in parietal cells under both acidic and neutral conditions. ![]() Vonoprazan does not require enteric coating as it is acid-stable, and it can be taken without food because it is quickly absorbed. It is currently indicated for the treatment of gastric and duodenal ulcers, reflux esophagitis, and prevention of low-dose aspirin- or nonsteroidal anti-inflammatory drug-related gastric and duodenal ulcer recurrence in Japan. ![]() Vonoprazan was recently innovated as a novel, orally active P-CAB. Potassium-competitive acid blockers (P-CABs) were developed and have beneficial effects including rapid, long-lasting, and reversible inhibition of the gastric hydrogen potassium ATPase, the proton pump of the stomach. Alternative formulations of conventional PPIs have been developed to overcome these problems however, these drugs have only introduced small advantages for controlling acid secretion compared to conventional PPIs. However, they have a number of limitations including slow onset of action, influence by cytochrome P450 polymorphisms, unsatisfactory effects at night, and instability in acidic conditions. Conventional proton pump inhibitors (PPIs) are used as a first-line therapy to treat acid-related diseases worldwide. ![]()
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