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新型质子泵抑制剂AGN 201904-Z可实现可预测的胃酸分泌长期抑制。

Predictable prolonged suppression of gastric acidity with a novel proton pump inhibitor, AGN 201904-Z.

作者信息

Hunt R H, Armstrong D, Yaghoobi M, James C, Chen Y, Leonard J, Shin J M, Lee E, Tang-Liu D, Sachs G

机构信息

Division of Gastroenterology, McMaster University and Hamilton Health Science Centre, Hamilton, ON, Canada.

出版信息

Aliment Pharmacol Ther. 2008 Jul;28(2):187-99. doi: 10.1111/j.1365-2036.2008.03725.x. Epub 2008 Apr 25.

DOI:10.1111/j.1365-2036.2008.03725.x
PMID:18445141
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4505925/
Abstract

BACKGROUND

AGN 201904-Z is a new, slowly absorbed, acid-stable pro-proton pump inhibitor (pro-PPI) rapidly converted to omeprazole in the systemic circulation giving a prolonged residence time.

AIM

To investigate pharmacodynamics and pharmacokinetics of AGN 201904-Z compared to esomeprazole.

METHODS

A randomized, open-label, parallel group, investigator-blinded intragastric pH study was conducted in 24 healthy Helicobacter pylori negative male volunteers. AGN 201904-Z enteric-coated capsules (600 mg/day) or esomeprazole delayed-release tablets (40 mg/day) were administered for 5 days. Twenty-four-hour intragastric pH recordings were acquired at baseline, days 1, 3 and 5 with blood levels of omeprazole, AGN 201904-Z and gastrin.

RESULTS

On day 1, median nocturnal pH and proportion of nocturnal time with pH >or=4 and 24-h and nocturnal time pH >or=5 were significantly higher with AGN 201904-Z than esomeprazole. At day 5, 24-h and median nocturnal pH were significantly higher for AGN 201904-Z than esomeprazole (P < 0.0001). There was also a marked reduction in periods of nocturnal pH <4.0. Area under curve of the AGN 201904-Z active metabolite (omeprazole) in the blood was twice that of esomeprazole at day 5.

CONCLUSIONS

AGN 201904-Z produced a significantly greater and more prolonged acid suppression than esomeprazole, and nocturnal acid suppression was more prolonged over all 5 days. AGN 201904-Z should provide true once-a-day treatment and better clinical efficacy than current PPIs.

摘要

背景

AGN 201904-Z是一种新型的、吸收缓慢、酸稳定的前体质子泵抑制剂（前体PPI），在体循环中迅速转化为奥美拉唑，从而延长了驻留时间。

目的

比较AGN 201904-Z与埃索美拉唑的药效学和药代动力学。

方法

对24名幽门螺杆菌阴性的健康男性志愿者进行了一项随机、开放标签、平行组、研究者设盲的胃内pH值研究。给予AGN 201904-Z肠溶胶囊（600毫克/天）或埃索美拉唑缓释片（40毫克/天），持续5天。在基线、第1天、第3天和第5天进行24小时胃内pH值记录，并检测奥美拉唑、AGN 201904-Z和胃泌素的血药浓度。

结果

在第1天，AGN 201904-Z组的夜间pH值中位数以及夜间pH≥4、24小时和夜间pH≥5的时间比例均显著高于埃索美拉唑组。在第5天，AGN 201904-Z组的24小时和夜间pH值中位数显著高于埃索美拉唑组（P<0.0001）。夜间pH<4.0的时间段也显著减少。在第5天，AGN 201904-Z活性代谢产物（奥美拉唑）的血药浓度曲线下面积是埃索美拉唑的两倍。

结论

AGN 201904-Z比埃索美拉唑产生了显著更大且更持久的抑酸作用，并且在整个5天内夜间抑酸作用更持久。AGN 201904-Z应能提供真正的每日一次治疗，并且比目前的质子泵抑制剂具有更好的临床疗效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b9e5/4505925/7deefbad141d/nihms68622f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b9e5/4505925/131993eb3f11/nihms68622f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b9e5/4505925/6138c90f0a32/nihms68622f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b9e5/4505925/fc358d7244b5/nihms68622f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b9e5/4505925/b1be0338f167/nihms68622f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b9e5/4505925/f4ba15bd728f/nihms68622f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b9e5/4505925/7deefbad141d/nihms68622f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b9e5/4505925/131993eb3f11/nihms68622f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b9e5/4505925/6138c90f0a32/nihms68622f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b9e5/4505925/fc358d7244b5/nihms68622f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b9e5/4505925/b1be0338f167/nihms68622f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b9e5/4505925/f4ba15bd728f/nihms68622f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b9e5/4505925/7deefbad141d/nihms68622f6.jpg

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