881681-00-1 Usage
Indications and Uses
Vanoprazan fumarate is a new oral gastric acidity drug developed by Takeda Pharmaceutical and Otsuka Pharmaceuticals. It is used to treat duodenal ulcers, gastric ulcers, reflux esophagitis, gastric ulcers or recurrent duodenal ulcers caused by low dosages of Aspirin, and Helicobacter pylori. It can also supplement treatment of gastric ulcers, duodenal ulcers, gastric MALT lymphoma, idiopathic thrombocytopenic purpura, early gastric cancer, and Helicobacter pylori infection gastritis.
Compared to traditional irreversible proton pump inhibitors (omeprazole, esomeprazole, etc.), Takecab has the following advantages:
1. Rapid effects, having the most drastic acid-suppressing effects on the first day of ingestion.
2. Oral intake, efficacy unaffected by gastric acid, does not require enteric administration.
Alleviated nighttime acid reflux.
Mechanisms of Action
Takecab (TAK-438) is a kind of potassium ion (K+) competitive acid blocker (P-CAB) and a reversible proton pump inhibitor. After this product enters the body, at the last step of gastric parietal cell acid secretion, it inhibits K+ ions from bonding with H+-K+-ATP enzymes (proton pump), thus stopping gastric acid secretion. It has a strong, lasting gastric acid suppression effect. TAK-438 is not mainly metabolized by protein CYP2C19, and it does not need to be activated by acid to inhibit protein pumps. As the drug enters the stomach at a high concentration, it will have the strongest suppressing effect at its first dosage, an effect which can last for up to 24 hours. TAK-438 is a stable acid, its formula is readily available and does not require optimized formulation (e.g. enteric coating), and its effective dosage amount does not vary dramatically between different patients.
Clinical Research
Compared to the traditional protein pump inhibitor Lansoprazole, Vonoprazan takes effect through competitive and reversible inhibition of K+ in protein pumps. Clinical and animal experiments show that Vonoprazan acts faster than PPI or H2 receptor blockers, has a stronger pH raising effect, can swiftly alleviate gastric symptoms, allows enzyme recovery after dissociation, and has few side effects. Multiple clinical trials have proved that in cases of erosive esophagitis, Vonoprazan prevents and treats gastric and duodenal ulcers. As a first-line response for eradicating helicobacter pylori, it has shown significant efficacy, higher than Lansoprazole and with minimal side effects.
Vonoprazan has high lipophilicity and dissociation constant, so in acidic environments, it can take effect without the activation of acid. Vonoprazan’s inhibition of protein pumps does not require acid activation. Upon entering the stomach at a high concentration in its first dosage, it produces its strongest inhibiting effect, which can last for 24 hours. Vonoprazan is a stable acid, and it can rapidly increase the pH in the stomach and suppress gastric acid.
Vonoprazan has minimal influence on other enzyme and bodily functions, making it very safe and tolerable. Traditional PPIs are metabolized by CYP2C19, while Vonoprazan is not. Its efficacy and required dosage do not differ dramatically in different patients, making it an advantageous individualized drug regimen for patients.
Patents
Chemical compound patent: 200680040789.7, application date: August 29, 2006, expiration date: August 29, 2026, legal status: holding rights.
Process patent: 201080018114.9, application date: February 24, 2013, expiration date: February 24, 2030. Legal status: In review – trial.
Composition patent: WO2014003199, application date: June 26, 2013, no Chinese patent.
Check Digit Verification of cas no
The CAS Registry Mumber 881681-00-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,8,1,6,8 and 1 respectively; the second part has 2 digits, 0 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 881681-00:
(8*8)+(7*8)+(6*1)+(5*6)+(4*8)+(3*1)+(2*0)+(1*0)=191
191 % 10 = 1
So 881681-00-1 is a valid CAS Registry Number.
881681-00-1Relevant articles and documents
Preparation method of funolasan fumarate
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, (2022/01/10)
The present invention provides a method for preparing funorasine fumarate, comprising the following steps: (1) the compound of formula I is azidine to give a compound of formula II.; (2) the compound of formula II. is cyclized with the compound of formula III. to give a compound of formula IV.; (3) the compound of formula IV. is condensed with a compound of formula VI. to give a compound of formula VII. compound; (4) a compound of formula VII. is deprotected with acid to obtain a vonorasin free base; (5) a vonorasin free base is salted with fumarate to give vonorasin fumarate. According to the method of the present invention to synthesize vonoracin fumarate, compared with the prior art, the total yield of vonora fumarate increased to more than 60%, and the yield has been greatly improved. Furthermore, compound formula IV. can be used as a new intermediate for the preparation of funolasine fumarate.
Vonoprazan fumarate intermediate and preparation method thereof
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, (2021/10/27)
The invention provides a vonoprazan fumarate intermediate compound as well as a preparation method and application thereof. Compared with the prior art, the technical scheme provided by the invention avoids the hydrogenation reaction operation with higher
Vonoprazan purification method
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Paragraph 0031; 0034, (2020/05/01)
The invention discloses a purification method of vonoprazan. The method comprises the following steps: preparing a refined solvent from a monohydric alcohol, formamide and water according to a certainratio; and purifying a vonoprazan crude product under t
