Vonolazan Fumarate API

Vonaprazan;5-(2-Fluorophenyl)-N-methyl-1-(3-pyridinylsulfonyl)-1H-pyrrole-3-methanamine2-butenedioate(Vonoprazan);1-[5-(2-fluorophenyl)-1-pyridin-3-Chemicalbookylsulfonylpyrrol-3-yl]-N-methylmethanamine;AK-438;Vonaprazan(TAK-438);vonoprazan(tak-438);Vonoprazanfumarate(TAK-438);vonoprazan(tak-438)1260141-27-2

Vonoprazan fumarate (TAK-438, Vonoprazanfumarate) is a new oral anti-gastric acid drug jointly launched by Takeda Pharmaceutical and Otsuka Pharmaceutical. [Registration Classification] Chemical Drug Class 3.1 [Indications] Used for the treatment of erosive esophagitis, gastric ulcer, and duodenal ulcer. On February 28, 2014, Takeda Pharmaceutical submitted a New Drug Application (NDA) for vonoprazan (TAK-438) to the Ministry of Labor, Health and Welfare (MHLW) of Japan. The submission of this NDA was based on good data from the Phase III clinical trial. Takeda Pharmaceutical has launched several Phase III clinical trials in Japan, aiming to investigate the efficacy of TAK-438 for erosive esophagitis, gastric ulcer, duodenal ulcer, and Helicobacter pylori eradication indications. In clinical trials, compared with the current proton pump inhibitors (PPIs), vonoprazan (TAK-438) has shown better efficacy in clinical trials because it does not have CYP2C19 metabolism: treating gastric ulcer/ten The efficacy of duodenal ulcer, reflux esophagitis, and pyloric screw eradication is better than that of lansoprazole, and it has good tolerance and safety. On December 26, 2014, Vonoprazan fumarate (TAK-438, Vonoprazanfumarate) was approved for marketing in Japan (trade name: Takecab) for the treatment of acid-related diseases. Compared with traditional irreversible proton pump inhibitors (such as omeprazole, esomeprazole, etc.), vonoprazan fumarate (Takecab) has the following advantages: ① It has a rapid onset of action and is effective on the first day of administration. It will achieve the maximum acid-suppressing effect of Chemicalbook; ② Oral administration is not affected by gastric acid damage, and does not need to be made into an enteric-coated administration form; ③ It has a certain effect on improving the phenomenon of acid breakthrough at night. Pharmacological effects Vonoprazan fumarate (TAK-438) is a potassium ion (K+) competitive acid blocker (P-CAB). It is a reversible proton pump inhibitor. After entering the human body, this product In the final step of cell acid secretion, by inhibiting the combination of K+ and H+-K+-ATPase (proton pump), the secretion of gastric acid is terminated and the acid-suppressing effect is achieved. This product has a strong and long-lasting inhibitory effect on gastric acid secretion. Currently, in Japan, proton pump inhibitors (PPIs) are widely prescribed for first-line treatment of acid-related diseases. However, PPIs do not always provide sufficient therapeutic effects. At the same time, the effect of inhibiting gastric acid secretion may vary from person to person. This is due to the fact that CYP-2C19, a protein involved in PPI metabolism, has genetic diversity in different individuals. morphology. However, TAK-438 is not mainly metabolized by CYP2C19. At the same time, TAK-438's inhibitory effect on proton pumps does not require activation by acid. The drug enters the stomach at a high concentration and can produce the maximum inhibitory effect when administered for the first time. And the effect lasts for 24 hours. TAK-438 is stable in acid, and the fast-acting formula is readily available. There is no need to optimize the formula design (such as enteric coating), and the difference in the effective dose among different patients is not significant. Based on these advantages, TAK-438 is expected to become a new therapeutic drug to solve the current problems in the treatment of acid-related diseases. This information was edited and compiled by Xiao Nan of Chemicalbook.

Vonoprazan fumarate (TAK-438, Vonoprazan fumarate) is a new oral anti-gastric acid drug jointly launched by Takeda Pharmaceutical and Otsuka Pharmaceutical.