iy-81149

Ilaprazole (IY-81149) is a proton pump inhibitor used in the treatment of dyspepsia gastroesophageal reflux disease (GORD/GERD) and duodenal ulcer. Studies also showed that Ilaprazole significantly prevented the development of reflux oesophagitis.

Ilaprazole sodium (IY-81149 sodium) , a substituted benzimidazole prodrug, is a selective and irreversible proton pump inhibitor. A weak base, Ilaprazole accumulates in the acidic environment of the secretory canaliculus of the gastric parietal cell where it is converted to an active sulfenamide form that binds to cysteine sulfhydryl groups on the luminal aspect of the proton pump hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase), thereby inhibiting the pump's activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production.

Ilaprazole (IY-81149) sodium hydrate is an orally active proton pump inhibitor that irreversibly inhibits H+ K+-ATPase in rabbit parietal cells with a dose-dependent IC50 of 6 μM. It is used in gastric ulcer research and acts as a potent inhibitor of T-lymphokine-activated killer cell-originated protein kinase (TOPK) [1] [2].

Ilaprazole sulfone, primarily metabolized by CYP3A4/5, constitutes the chief metabolite of Ilaprazole (IY-81149), an orally active proton pump inhibitor [1].