Effects of IY-81149, a Newly Developed Proton Pump Inhibitor, on Gastric Acid Secretion in vitro and in vivo | Semantic Scholar (2024)

The systemic availability of CDRI-85/92 decreased from 6111 to 3 463 ng · h/ml after the ester prodrug administration, and this decrease in systemic availability could be due to its higher clearance after its esterProdrug administration.

The result of the in silico prediction indicates that all the new metabolites of ilaprazole showed the potential ability to inhibit H+/K+-ATPase activity.

This mechanism-based PK/PD model provided a potential strategy to accelerate the development of novel PPIs by waiving the unnecessary clinical trials and predicted the PK and PD profile of ilaprazole in healthy subjects and patients with duodenal ulcers receiving wide range dose regimens.

In anesthetized rats, the inhibitory effect of intravenous ilaprazole on histamine-induced acid secretion is faster and longer-lasting than that of intraduodenal ilapazole.

The structural elucidation of urinary metabolites of ilaprazole in human was described byHPLC-ESI-MS/MS and stopped-flow HPLC-NMR experiments and testified that HPLCs and NMR could be widely applied in detection and identification of novel metabolites.

In healthy volunteers, as well as in patients with gastric or duodenal ulcers, ilaprazole has not shown clinically relevant changes in hematology and biochemistry testing, nor significant treatment-related adverse symptoms, so studies comparing the clinical pharmaco*kinetics and pharmacodynamics of ilapazole with those of second-generation PPIs are insufficient.

The broad therapeutic value of prokinetics in GORD does, however, seem very limited in terms of efficacy with respect to oesophageal motility and acid exposure, and further research is necessary to better understand the complex mechanisms involved in oesophileal sensitivity and mucosal defence.

The rationale behind this approach, the potential selectivity in targeting tumor acidity, and the ability to inhibit mechanism pivotal for cancer homeostasis are explained and practical evidence is provided.

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It is shown that H 149/94 inhibits (H+ + K+)ATPase, which may explain its inhibitory action on acid secretion in vitro and in vivo and may be a highly selective clinical means of suppressing the acid secretory process.

The gastric H+,K+ ATPase--the gastric acid pump--is the molecular target for the class of antisecretory drugs called the proton-pump inhibitors (PPIs), which show synergism with either amoxicillin or clari- thromycin in eradicating Helicobacter pylori.

Data indicate that in this in vitro system parietal cells account for most of the increase in oxygen uptake produced by exposure to gastric secretagogues and that histamine, gastrin, and carbamylcholine each independently stimulate oxygen uptake by the parietal cell.

The parietal cell occupies a unique niche among eukaryotic cells in that it develops a proton gradient across the membrane of the secretory canaliculus, such that the acid compartment has a pH of less than 4.

The stomach of the rat anaesthetized with urethane is perfused with a dilute sodium hydroxide solution by way of the oesophagus and the pH of the fluid emerging from a cannula in the pylorus is registered graphically.

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