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)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03808493||Completed||Drug: TAK-438 OD|Drug: TAK-438||Japanese Healthy Adult Male||Takeda||January 30 2019||Phase 1|
|NCT03456960||Completed||Drug: TAK-438ASA|Drug: TAK-438|Drug: Aspirin||Japanese Healthy Adult Male||Takeda||March 8 2018||Phase 1|
|NCT03085836||Completed||Drug: TAK-438||Healthy Participants||Takeda||April 19 2017||Phase 1|
|NCT02774902||Completed||Drug: TAK-438|Drug: Clarithromycin||Healthy Volunteers||Takeda||August 2010||Phase 1|
|NCT02141711||Completed||Drug: TAK-438|Drug: TAK-438 Placebo||Erosive Esophagitis(EE)|Gastroesophageal Reflux Disease (GERD)||Takeda||October 2008||Phase 1|
|NCT02123953||Completed||Drug: TAK-438|Drug: TAK-438 Placebo||Dose Finding Study||Takeda||October 2008||Phase 1|
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