01
Vonoprazan fumarate 1260141-27-2
Product Specification
Appearance: |
White to off-white powder |
Water： |
NMT 0.5% |
Residue on ignition： |
NMT 0.2% |
Heavy metals ： |
NMT 20ppm |
Related substance(HPLC)： |
Impurity A NMT 0.1% 、Impurity B NMT 0.1%、Impurity C NMT 0.1%、Any other individual impurity NMT 0.1%、Total impurities NMT 0.5% |
Fumarate： |
23.9~26.4% |
Purity： |
NLT 99.5% |
description1
PRODUCT DESCRIPTION
Vonoprazan fumarate (Takecab®), discovered and developed by Takeda and Otsuka, was approved by the PMDA of Japan in December 2014, and is indicated for the treatment of gastric ulcer, duodenal ulcer and reflux esophagitis. Vonoprazan fumarate has a novel mechanism of action called potassium-competitive acid blockers, which competitively inhibit the binding of potassium ions to H+, K+-ATPase (also known as the proton pump) in the final step of gastric acid secretion in gastric parietal cells. Vonoprazan does not inhibit Na+, K+-ATPase activity even at concentrations 500 times higher than that of their IC50 values against gastric H+, K+-ATPase activity. Furthermore, the drug is unaffected by the gastric secretory state, unlike PPIs.
Vonoprazan is a selective, reversible, and potassium-competitive proton pump inhibitor that inhibits gastric H+/K+ ATPase (IC50 = 17 nM) but does not inhibit porcine Na+/K+ ATPase activity when used at a concentration of 10 μM. It maintains its inhibitory effect in both weakly acidic (pH 6.5) and neutral (pH 7.5) conditions with IC50 values of 19 and 28 nM, respectively. In vivo, vonoprazan (1, 2, and 4 mg/kg) inhibits histamine-stimulated acid secretion in a dose-dependent manner in rats, with complete inhibition when administered at a dose of 4 mg/kg. It also inhibits acid secretion for more than 48 hours in dogs when administered at doses ranging from 0.1 to 1 mg/kg.
Vonoprazan fumarate is an oral, newly synthesised potassium-competitive acid blocker (P-CAB) with antisecretory activity. It is also a proton pump inhibitor (PPI) reversibly inhibiting H+/K+, ATPase. It is mainly used in the treatment of acid-related diseases such as GERD and peptic ulcer disease.Vonoprazan is used to treat an infection caused by the bacteria H. pylori. This bacteria can cause stomach/intestinal ulcers and irritation/swelling of the lining of the stomach. It may also increase the risk of stomach cancer. Treating the infection will help the ulcers get better and reduces the risk of serious damage to the lining of the stomach/intestines (such as bleeding, tearing).Vonoprazan is an acid blocker. It works by blocking acid production in the stomach. Decreasing excess stomach acid can help ulcers heal. Amoxicillin is an antibiotic used to treat a wide variety of bacterial infections (including H. pylori). Treating the infection helps the ulcers heal and reduces the risk of ulcers returning. Amoxicillin is a penicillin-type antibiotic. It works by stopping the growth of bacteria. Amoxicillin treats only bacterial infections. It will not work for viral infections (such as common cold, flu).