Leminoprazole

Leminoprazole is an orally available H+,K(+)-ATPase inhibitor that protects gastric mucosal cells from various cellular damages.

Leminoprazole inhibited H+, K(+)-ATPase activity in a concentration-dependent manner, with an IC₅₀ value of 31 μM at pH 7.4.^[1]

Leminoprazole, when given orally at doses of 10-100 mg/kg, was able to dose-dependently inhibit H+, K(+)-ATPase activity at 3 and 6 hours after administration. Specifically, Leminoprazole (60 mg/kg, p.o.) inhibited H+, K(+)-ATPase for a much longer duration than omeprazole (30 mg/kg, p.o.). In pylorus ligated rats, the inhibitory effect of Leminoprazole on gastric acid secretion and its inhibitory rate on H+, K(+)-ATPase activity showed a good correlation, suggesting that the inhibitory efficacy of Leminoprazole in inhibiting gastric acid secretion via H+, K(+)-ATPase activity is comparable to that of omeprazole. The inhibitory effect was comparable to that of omeprazole. In addition, Leminoprazole (100 mg/kg) directly inhibited H+, K(+)-ATPase activity even when administered intragastrically after pyloric ligation, demonstrating the ability of this compound to inhibit H+, K(+)-ATPase activity directly from the gastric lumen. Further studies showed that continuous administration of Leminoprazole (100 mg/kg, p.o.) for 2 or 4 weeks had the same inhibitory effect on H+, K(+)-ATPase as a single dose.

References:
1.Matsukura H, et al. Effect of a new antiulcer drug, leminoprazole, on the gastric mucosal H+,K(+)-ATPase activity in rats. Nihon Yakurigaku Zasshi. 1994 Aug;104(2):91-100.