TAK-438 Free Base is a blocker of potassium-competitiveproton pump that reversibly inhibits H+/K+ATPase with IC50 of 17 nM at pH 6.5 while do not affect on Na+/K+ATPase activity. It has been used to treatment of erosive esophagitis and gastroduodenal ulcer.
TAK-438 free base (Vonoprazan) is an orally active potassium-competitive acid blocker which inhibits H+, K+-ATPase activity with an IC50 of 19 nM. It is a novel potassium-competitive acid blocker that inhibits gastric H(+), K(+)-ATPase. In healthy Japanese male subjects, triple therapy with vonoprazan-amoxicillin-clarithromycin increased vonoprazan and clarithromycin exposure. The safety and tolerability profile of triple therapy with vonoprazan-amoxicillin-clarithromycin or vonoprazan-amoxicillin-metronidazole was favorable in this population[3]. The healing rate of GERD (gastroesophageal reflux disease) and gastric ulcers by vonoprazan is more than 95 and 90%, respectively; also, it is effective in curing PPI (proton pump inhibitors)-resistant GERD. It is also effective in the eradication of clarithromycin-resistant H. pylori strains. All of these short-term studies show vonoprazan is safe and well-tolerated[4]. Vonoprazan (10 and 20 mg) was as effective as lansoprazole (15 mg) in preventing peptic ulcer recurrence during LDA (low-dose aspirin) therapy, had a similar long-term safety profile and was well tolerated[5].
搜索
