Vonoprazan Fumarate (TAK-438)
Molecular Weight(MW): 461.46
Vonoprazan Fumarate (TAK-438) is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase with IC50 of 19 nM (pH 6.5), controls gastric acid secretion. Phase 3.
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Choose Selective Potassium Channel Inhibitors
|Description||Vonoprazan Fumarate (TAK-438) is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase with IC50 of 19 nM (pH 6.5), controls gastric acid secretion. Phase 3.|
|Features||Capable of inhibiting H+, K+-ATPase under acidic or neutral conditions.|
TAK-438 is a pyrrole derivative with a chemical structure that is completely different from the P-CABs developed to date. TAK-438 inhibits gastric H+, K+-ATPase activity in a concentration-dependent manner. Under neutral conditions (pH 7.5), the inhibitory activity of TAK-438 is almost the same as that under weakly acidic conditions (pH 6.5). TAK-438 does not inhibit Na+, K+-ATPase activity even at concentration 500 times higher than their IC50 values against gastric H+,K+-ATPase activity. TAK-438 inhibits gastric H+, K+-ATPase in a K+-competitive manner with Ki of 3 nM. 
|In vivo||TAK-438 inhibits basal gastric acid secretion in a dose-dependent manner, and the ID50 value is 1.26 mg/kg . Intravenous administration of TAK-438 dose-dependently increases the pH of the gastric perfusate, and the increase in pH is sustained for 5 h after administration. At the 1 mg/kg dose, the pH plateaues 90 min after administration, and the highest pH value reached is 5.9.  In addition, TAK-438 shows a potent and longer-lasting inhibitory effect on the histamine-stimulated gastric acid secretion in rats and dogs. TAK-438 shows significant antisecretory activity through high accumulation and slow clearance from the gastric tissue. TAK-438 is unaffected by the gastric secretory state, unlike PPIs. |
|In vitro||DMSO||62 mg/mL (134.35 mM)|
|In vivo||Add solvents individually and in order:
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03050307||Not yet recruiting||Gastric Ulcer|Peptic Ulcer|Gastrointestinal Diseases|Digestive System Diseases|Lansoprazole|Anti-Ulcer Agents|Gastrointestinal Agents|Proton Pump Inhibitors|Enzyme Inhibitors|Molecular Mechanisms of Pharmacological Action||Takeda||April 2017||Phase 3|
|NCT03050359||Not yet recruiting||Duodenal Ulcer||Takeda||April 2017||Phase 3|
|NCT02954848||Recruiting||Non-erosive Gastroesophageal Reflux Disease||Takeda||December 2016||Phase 3|
|NCT02892409||Recruiting||Helicobacter Pylori||Takeda||September 2016||Phase 1|
|NCT01630746||Completed||Erosive Esophagitis||Takeda||July 2012||Phase 3|
|NCT01568398||Completed||Gastric Ulcer|Duodenal Ulcer||Takeda||May 2012||Phase 3|
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