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更新于：2026-08-27
Ilaprazole
艾普拉唑
更新于：2026-08-27
概要
基本信息
药物类型 小分子化药 |
别名 Aldenon、Aldenonc、IY-NT-R + [7] |
作用方式 抑制剂 |
作用机制 质子泵抑制剂 |
原研机构 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (2007-12-11), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C19H18N4O2S |
InChIKeyHRRXCXABAPSOCP-UHFFFAOYSA-N |
CAS号172152-36-2 |
关联
110
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艾普拉唑肠溶片在健康受试者中的单中心、随机、开放、单剂量、两制剂、四周期、两序列完全重复交叉的空腹及餐后给药人体生物等效性研究
CTR20260830
艾普拉唑肠溶片在健康试验参与者中空腹/餐后状态下的单剂量、随机、开放、四周期、两制剂、完全重复交叉设计的生物等效性试验
100 项与 艾普拉唑 相关的临床结果
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100 项与 艾普拉唑 相关的转化医学
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100 项与 艾普拉唑 相关的专利（医药）
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146
项与 艾普拉唑 相关的文献（医药）2026-04-09ACS Medicinal Chemistry Letters
Repurposing Ilaprazole as a PP5 TPR Domain Binder with Modulatory Effects on MAPK Signaling
Article
作者: He, Yanyi ; Huang, Qifei ; Zhang, Qiuyue ; Gu, Jinying ; Wang, Lei ; Hua, Liwen ; Zhai, Daichao ; You, Qidong ; Pei, Jiayue
Small-molecule modulators targeting the N-terminal tetratricopeptide repeat (TPR) domain of protein phosphatase 5 (PP5) remain largely unexplored. Here, we report the repurposing of ilaprazole as a PP5 TPR domain binder identified via a fluorescence polarization-based competitive screen. Biophysical assays and molecular docking supported the interaction within the PP5 TPR binding pocket, revealing key structural features distinguishing ilaprazole from related proton pump inhibitors. In KRAS mutant colorectal cancer cells, ilaprazole engaged cellular PP5, leading to reduced RAF stability and suppressed mitogen-activated protein kinase (MAPK) signaling. While exhibiting minimal single-agent effects, ilaprazole sensitized cells to the MEK inhibitor binimetinib. These results validate the PP5 TPR domain as a druggable site and establish ilaprazole as a lead scaffold for pharmacological modulation of PP5-associated MAPK signaling.
2026-03-01Clinical Pharmacology in Drug Development
Pharmacokinetics and Bioequivalence of Ilaprazole Enteric‐Coated Tablets in Healthy Chinese Volunteers: A Two‐Sequence, Four‐Period, Fully Replicated Crossover Study
Article
作者: Du, Lijie ; Gan, Fangliang ; Yang, Jiamin ; Li, Li ; Zhang, Yi
Abstract:
Ilaprazole enteric‐coated tablets are a novel proton pump inhibitor primarily used for the treatment of gastroesophageal reflux disease, with metabolism not affected by CYP2C19 genetic polymorphism. This study evaluated the pharmacokinetics and bioequivalence of two formulations of ilaprazole enteric‐coated tablets in Chinese healthy volunteers under fasting and fed conditions using a single‐center, randomized, open‐label, single‐dose, two‐formulation, four‐period, two‐sequence, fully replicated crossover design. A total of 72 volunteers were enrolled, with 36 in each group. In the fasting group, volunteers received a single dose of 5 mg of the test or reference formulation in each period, while in the fed group, a high‐fat meal was consumed 30 min before drug administration. Blood samples were collected within 36 h postdose, and plasma concentrations of ilaprazole were analyzed using ultra‐performance liquid chromatography‐tandem mass spectrometry. The geometric means and 90% confidence intervals of AUC
0–t
, AUC
0–∞
, and C
max
for both fasting and fed conditions were within the 80%–125% bioequivalence range, and the upper limit of the one‐sided 95% confidence interval was ≤0. Both formulations demonstrated bioequivalence under these conditions, with no serious adverse reactions observed.
2026-02-01Arab Journal of Gastroenterology
Assessment of diverse proton pump inhibitor combined with bismuth quadruple regimens and risk factors for Helicobacter pylori eradication in China: A retrospective single-center study
Article
作者: Zhang, Yaqiong ; Yang, Mengyuan ; Zhao, Xiaolin ; Fan, Chanjuan ; Liu, Yang ; Cheng, Jianping
BACKGROUND AND STUDY AIMS:
Falling eradication rates of Helicobacter pylori (H. Pylori) have prompted changes in the first-line bismuth-containing quadruple therapy. This study aimed to assess the effectiveness of different proton-pump inhibitor (PPI) based quadruple regimens for H. pylori eradication.
PATIENTS AND METHODS:
Electronic records were examined to acquire information on H. pylori-positive patients treated with a 14-day bismuth-containing quadruple regimen (PPIs, amoxicillin, clarithromycin, and bismuth). Patient demographics and eradication regimen data were also analyzed. Four groups were formed based on the different PPIs: ilaprazole, esomeprazole, omeprazole, and rabeprazole groups. Eradication rates were calculated, and the effectiveness of the treatment regimens was compared.
RESULTS:
A total of 2637 patients were included, comprising 1469 males and 1168 females. Of these, 22.4 % (n = 590) were treated with an ilaprazole-based quadruple regimen, 33.8 % (n = 892) with an esomeprazole-based regimen, 16.6 % (n = 439) with an omeprazole-based regimen, and 27.2 % (n = 716) with a rabeprazole-based regimen. Eradication rates were significantly higher in the esomeprazole-based regimen than in the ilaprazole-, omeprazole-, and rabeprazole-based regimens (75.2 % vs. 65.8 % vs. 65.4 % vs. 70.9 %, P = 0.001).
CONCLUSIONS:
The eradication rates across various PPI-based quadruple regimens were comparable; however, the regimen comprising amoxicillin and clarithromycin demonstrated low efficacy and is not advised in settings with high clarithromycin resistance. Among the effective therapeutic regimens, the esomeprazole-based regimen exhibited a slightly higher eradication rate.
100 项与 艾普拉唑 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 反流性食管炎 | 印尼 | 2022-09-27 | |
| 胃食管反流 | 中国 | 2015-04-16 | |
| 糜烂性食管炎 | 韩国 | 2008-10-28 | |
| 胃溃疡 | 韩国 | 2008-10-28 | |
| 十二指肠溃疡 | 中国 | 2007-12-11 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 非糜烂性胃食管反流病 | 临床3期 | 韩国 | 2018-10-31 | |
| 非糜烂性反流病 | 临床3期 | 韩国 | 2018-10-31 | |
| 幽门螺杆菌引起的十二指肠溃疡 | 临床3期 | 韩国 | 2012-12-01 | |
| 消化性溃疡出血 | 临床2期 | - | 2014-02-01 | |
| 幽门螺杆菌感染 | 临床申请批准 | 中国 | 2022-11-01 |
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临床结果
临床结果
适应症
分期
评价
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临床4期 | 480 | Ilaprazole 10mg bid + amoxicillin 1g tid | 憲蓋壓遞遞艱鬱膚膚憲(淵構淵鹽醖鏇醖選廠遞) = 廠鬱鬱築鏇夢願範繭築 蓋鑰淵壓顧壓積鏇鹽鏇 (鹹選夢窪鑰鹹壓範淵夢 ) 更多 | 积极 | 2026-05-02 | ||
Vonoprazan 20mg bid + amoxicillin 1g tid | 憲蓋壓遞遞艱鬱膚膚憲(淵構淵鹽醖鏇醖選廠遞) = 餘積觸齋鏇遞廠觸膚憲 蓋鑰淵壓顧壓積鏇鹽鏇 (鹹選夢窪鑰鹹壓範淵夢 ) 更多 | ||||||
临床4期 | 176 | 簾蓋蓋鑰壓廠鑰衊網憲(築餘製膚願齋觸繭廠蓋) = 鬱壓鏇獵繭積壓繭衊繭 鹽壓蓋艱網鹹觸願繭窪 (選選範簾衊遞鹽觸蓋製 ) 更多 | 积极 | 2019-05-01 | |||
rabeprazole | 簾蓋蓋鑰壓廠鑰衊網憲(築餘製膚願齋觸繭廠蓋) = 醖願獵鹽衊鹽醖糧願遞 鹽壓蓋艱網鹹觸願繭窪 (選選範簾衊遞鹽觸蓋製 ) 更多 | ||||||
临床3期 | 537 | 鏇膚遞網窪壓獵糧觸獵(鹹選餘憲醖餘遞積窪築) = 糧簾簾艱構淵廠選齋願 積夢廠製憲艱選蓋膚構 (積淵網蓋鏇遞獵窪窪網 ) 更多 | 相似 | 2018-05-01 | |||
鏇膚遞網窪壓獵糧觸獵(鹹選餘憲醖餘遞積窪築) = 艱鹹襯窪網襯鹽壓艱餘 積夢廠製憲艱選蓋膚構 (積淵網蓋鏇遞獵窪窪網 ) 更多 | |||||||
临床2期 | - | 衊壓夢構壓鬱襯憲鹹選(鹹網鏇衊簾醖鹹鏇憲醖) = 齋選鏇製夢憲襯衊選簾 鹽積製憲廠鏇窪鑰製積 (糧襯顧壓鹹願夢鹽壓顧, (86.73%)) 更多 | - | 2016-12-01 | |||
衊壓夢構壓鬱襯憲鹹選(鹹網鏇衊簾醖鹹鏇憲醖) = 鹽範積夢鏇蓋淵築遞襯 鹽積製憲廠鏇窪鑰製積 (糧襯顧壓鹹願夢鹽壓顧, (81.40%)) 更多 | |||||||
临床3期 | 494 | Ilaprazole 10mg/d | 網遞簾醖繭積衊構範鑰(鹽蓋壓醖膚壓範醖鬱繭) = 鹽範選鹽壓襯顧襯獵獵 遞膚鹽觸鏇鬱選窪顧觸 (淵艱築鑰範淵淵製艱鑰 ) | 积极 | 2012-01-01 | ||
Omeprazole 20mg/d | 網遞簾醖繭積衊構範鑰(鹽蓋壓醖膚壓範醖鬱繭) = 網遞襯廠製鑰鏇淵顧鏇 遞膚鹽觸鏇鬱選窪顧觸 (淵艱築鑰範淵淵製艱鑰 ) | ||||||
临床2期 | 235 | Ilaprazole 5 mg | 製觸窪鬱顧廠艱衊構鑰(繭鹽鬱淵顧網襯觸襯鬱) = 鹽糧鑰範餘鑰糧膚衊獵 繭醖餘鏇鏇繭醖選壓鑰 (築窪壓窪獵窪網餘鬱淵 ) | - | 2011-04-01 | ||
Ilaprazole 10 mg | 製觸窪鬱顧廠艱衊構鑰(繭鹽鬱淵顧網襯觸襯鬱) = 鹽襯醖構範淵鏇壓壓觸 繭醖餘鏇鏇繭醖選壓鑰 (築窪壓窪獵窪網餘鬱淵 ) |
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