Chemical Property of TAK-438
Chemical Property:
- PSA：146.97000
- LogP:3.82910
- Solubility.:insoluble in H2O; insoluble in EtOH; ≥18.9 mg/mL in DMSO
- Purity/Quality:
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99%, *data from raw suppliers
TAK 438 *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
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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.
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Uses
Vonoprazan Fumarate is a novel potassium-?competitive acid blocker for the treatment of acid-?related diseases.
