The gastric H+,K+-ATPase, composed of the catalytic α subunit and the structural β subunit, is responsible for gastric acid secretion[1]. Ilaprazole is a novel proton pump inhibitor which inhibits H+,K+-ATPase with an IC50 of 6 μM. Ilaprazole is also a potent T-cell-originated protein kinase (TOPK; playing an indispensable role in the mitosis of cancer cells) inhibitor with a Kd of 111 μM[2]. On cumulation of 14C-aminopyrine in histamine stimulated parietal cells, the IC50 of ilaprazole was 9.0 nM. In rats, ilaprazole given intraduodenally immediately after pylorus ligation, dose-dependently inhibited gastric acid secretion. At 30 mg/kg, it showed 93% and 73% inhibition on acid output and volume compared to control, respectively. In Heidenhain pouch dog, the acid output was blocked dose-dependently by intravenous administration of ilaprazole at doses of 0.3 and 1 mg/kg[3].
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