881681-00-1
TAK-438 (free base)
CAS: 881681-00-1
Molecular Formula: C17H16FN3O2S
881681-00-1 - Names and Identifiers
881681-00-1 - Physico-chemical Properties
| Molecular Formula | C17H16FN3O2S |
| Molar Mass | 345.39 |
| Density | 1.31±0.1 g/cm3(Predicted) |
| Boling Point | 530.3±60.0 °C(Predicted) |
| Solubility | DMSO: ≥ 33 mg/mL |
| Appearance | Solid |
| Color | Pale Yellow to Light Yellow Sticky to |
| pKa | 9.06±0.10(Predicted) |
| Storage Condition | Hygroscopic, -20°C Freezer, Under inert atmosphere |
| Stability | Hygroscopic |
881681-00-1 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.895 ml | 14.476 ml | 28.953 ml |
| 5 mM | 0.579 ml | 2.895 ml | 5.791 ml |
| 10 mM | 0.29 ml | 1.448 ml | 2.895 ml |
| 5 mM | 0.058 ml | 0.29 ml | 0.579 ml |
Last Update：2024-01-02 23:10:35
881681-00-1 - Reference Information
| antacid drugs | Vonoprazan fumarate (TAK-438, Vonoprazan fumarate) it is a new type of oral anti-gastric acid drug launched by the cooperation of Wutian pharmaceutical and Otsuka Pharmaceutical. [registration classification] Drugs category 3.1 [indications] for the treatment of erosive esophagitis, gastric ulcer, duodenal ulcer. on 28-24-14-28-14-14-29 (TAK-438) New Drug Application (NDA) submitted to the Ministry of Labor, Health and Welfare (MHLW) of Japan, the submission of this new drug application is based on good data from Phase III clinical trials. Several Phase III clinical trials have been carried out in Japan to investigate the efficacy TAK-438 for erosive esophagitis, gastric ulcer, duodenal ulcer, Helicobacter pylori eradication indications. In clinical trials, compared with the current proton pump inhibitors (PPIs), vonoprazan (TAK-438) does not have CYP2C19 metabolism, so it shows better efficacy in clinical trials: the treatment of gastric ulcer/duodenal ulcer, reflux esophagitis, eradication of Helicobacter pylori and other efficacy is better than lansoprazole, and has good tolerability and safety. Vonoprazan fumarate (TAK-438, Vonoprazan fumarate) was approved for marketing in Japan under the trade name Takecab for the treatment of acid-related diseases. Compared with the traditional irreversible proton pump inhibitors (such as omeprazole, esomeprazole, etc.), vonoprazan fumarate (Takecab) has the following advantages: ①, the first day of administration will achieve the maximum acid suppression effect; (2) oral administration, not affected by gastric acid damage, do not need to be made into the form of enteric administration; (3) it can improve the acid breakthrough phenomenon at night. |
| pharmacological action | vonoprazan fumarate (TAK-438) is a potassium (K) competitive acid blocker (P-CAB), is a reversible proton pump inhibitor, this product enters the human body, in the last step of the gastric parietal cell acid secretion, by inhibiting the combination of K and H -K-ATPase (proton pump), termination of gastric acid secretion, acid suppression effect, this product has a strong, lasting inhibition of gastric acid secretion. currently, proton pump inhibitors (PPIs) have been widely prescribed for the first-line treatment of acid-related diseases in Japan. But PPI is not always able to provide adequate efficacy, at the same time, the inhibitory effect of gastric acid secretion may also vary from person to person, this is because of a protein involved in the metabolism of PPI CYP-2C19, the coding gene has gene polymorphism in different individuals. but TAK-438 is not mainly metabolized by CYP2C19, while TAK-438 inhibition of the proton pump, without acid activation, the drug enters the stomach in high concentrations, at the first dose, the maximum inhibitory effect can be produced, and the effect can last for 24 hours. TAK-438 is stable in acid, while the rapid-acting formula is ready, without the need to optimize the formulation design (such as enteric coating), and the difference in the effective dose is not significant in different patients. 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. |
| clinical evaluation | 1, compared with the traditional Proton Pump Inhibitor Lansoprazole, Vonoprazan, reversible Inhibition of K in the proton pump, clinical and animal experiments show that vonoprazan is faster than PPI or H2 receptor blockers, the role of increasing pH is stronger, can quickly relieve gastrointestinal symptoms, after dissociation of the enzyme activity recovery, less adverse reactions, several clinical trials have confirmed that vonoprazan for erosive esophagitis, prevention and treatment of gastric, duodenal ulcer, as a first-line treatment, eradication of Helicobacter pylori has a significant therapeutic effect, the curative effect is higher than that of lansoprazole, and the adverse reaction is small. 2, vonoprazan has high lipophilicity and high dissociation constant. In acidic environment, it can work without acid activation. The inhibition of the proton pump by vonoprazan does not require the activation of the acid, and enters the stomach in high concentration. The first administration can produce the maximum inhibitory effect and can last 24 hours. Vonoprazan is stable in acid, can rapidly increase the pH value in the stomach, and exerts acid suppression effect. 3. At the therapeutic dose, vonoprazan has little effect on other enzymes, has little effect on the physiological function of the body, has good safety and is easier to tolerate. Traditional PPI is metabolized by CYP2C19, while vonoprazan is not mainly metabolized by CYP2C19. The difference in efficacy and effective dose among different patients is not significant, which can better meet the patient's individualized medication regimen. |
| indications | treatment of duodenal ulcer, gastric ulcer and reflux esophagitis, gastric ulcer caused by low-dose aspirin or recurrent duodenal ulcer. eradication of Helicobacter pylori, adjuvant treatment of the following diseases: gastric ulcer, duodenal ulcer, gastric MALT lymphoma, idiopathic thrombocytopenic purpura, early gastric cancer, Helicobacter pylori infection gastritis. |
| synthesis method | Figure 1 shows the new oral anti-gastric acid drug Vonoprazan the chemical synthesis roadmap. |
| patent | compound patent: 200680040789.7, application date: 29-Aug -2006, expiration date: 29-Aug -2026, legal status: right. process patent: 201080018114.9, application date: 02-month 24, expiration date: 20-month 24, 30, legal status: In-trial-actual trial. Patent for composition: WO2014003199, date of application: 26/2013, no Chinese patent. |
| Market outlook | vonoprazan is undoubtedly a gold-sucking anti-gastric acid drug, however, because of the failure of research and development of P-CAB drugs and the fierce competition of PPIs in the market, some people are not optimistic about this drug. Even so, domestic companies are still in the first time to seize the copy of the Declaration of vonoprazan. This is another group of 3.1 Drugs reported by an original research enterprise in China shortly after approval. It has been reported from the first time that the original research drug was listed in the world to the domestic generic drug declaration, not more than half a year before and after, in addition to the 3.1 class of new drugs reported boom, more and more fast to grab the copy of the declaration has become another hot trend. |
Last Update：2024-04-09 20:52:54
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Product Name: TAK-438 (free base) Visit Supplier Webpage Request for quotation
CAS: 881681-00-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 881681-00-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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