预约演示
更新于：2026-10-27
Ilaprazole
艾普拉唑
更新于：2026-10-27
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
项与 艾普拉唑 相关的临床试验CTR20263115
艾普拉唑肠溶片在健康试验参与者中空腹状态下的单剂量、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
CTR20261472
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
CTR20261400
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
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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150
项与 艾普拉唑 相关的文献（医药）2026-10-01BIOORGANIC CHEMISTRY
Rabeprazole exhibits broad-spectrum fusion inhibition against Nipah pseudovirus and authentic HCoV-OC43 and RSV
Article
作者: Wang, Boxuan ; Liang, Ze ; Yan, Lei ; Shen, Yunyue ; Liu, Lili ; Yang, Guang ; Li, Jie
Rabeprazole was previously defined as a small-molecule fusion inhibitor that binds the conserved hydrophobic HR1 groove of the SARS-CoV-2 spike and blocks six-helix bundle assembly. Here, we expand its antiviral spectrum and demonstrate potent activity against Nipah virus pseudotype, HCoV-229E, and RSV. Using SPR, pseudovirus neutralization, docking, and 100-ns MD simulations, we validated binding of Rabeprazole to the HR1 domains of NiV F glycoprotein and HCoV-229E spike, with a conserved fusion-inhibitory mechanism. Systematic structure-activity relationship (SAR) profiling among clinically approved PPIs revealed that Ilaprazole and Lansoprazole exhibited stronger anti-NiV potency than Rabeprazole, while Rabeprazole sulfide showed enhanced antiviral activity relative to the parent compound. Rabeprazole also inhibited live RSV and HCoV-229E infection in a dose-dependent manner. Collectively, these findings establish the HR1 groove as a druggable pan-viral target and validate benzimidazole-based PPIs as a versatile scaffold for developing orally available, broad-spectrum antivirals against phylogenetically distinct enveloped viruses that rely on class I fusion machinery.
2026-09-18CURRENT DRUG TARGETS
Cytochrome P450 Enzymes in the Metabolism of Proton Pump Inhibitors: Implications for the Treatment of Peptic Ulcers
Article
作者: Sharma, Chetan Banbarilal ; Prajapati, Shatrudhan ; Yadav, Shikha
Introduction::
Peptic Ulcer Disease (PUD) remains a prevalent gastrointestinal condition
primarily caused by Helicobacter pylori infection and chronic NSAID use. Proton Pump Inhibitors
(PPIs) are the mainstay therapy, promoting mucosal healing through profound gastric acid suppression.
However, variable clinical outcomes are frequently observed, largely influenced by individual
differences in PPI metabolism mediated by cytochrome P450 (CYP450) enzymes, especially
CYP2C19 and CYP3A4.
Methods::
The review is a critical analysis of the evidence on PPI pharmacokinetics, pharmacogenomics,
and drug-drug interactions based on a structured search of PubMed, Scopus, and
Web of Science, with predetermined inclusion and exclusion criteria to ensure equal consideration of
studies on the topic.
Results::
Genetic polymorphisms in CYP2C19 create distinct metabolizer phenotypes—poor, intermediate,
extensive, and ultrarapid—that markedly influence PPI plasma levels, intragastric pH control,
and ulcer healing rates. Poor metabolizers exhibit superior healing due to prolonged acid suppression,
while ultrarapid metabolizers are prone to treatment failure. Rabeprazole and ilaprazole,
showing minimal CYP2C19 dependence, provide consistent efficacy across genotypes and reduced
drug interaction potential.
Discussion::
Pharmacogenomic variability in CYP2C19 significantly affects therapeutic response and
adverse outcomes. Personalized therapy based on genotype can optimize PPI efficacy, minimize
toxicity, and reduce drug–drug interactions, particularly with agents such as clopidogrel.
Conclusion::
Incorporating CYP2C19 genotyping and pharmacogenomic data into clinical decisionmaking
may improve treatment individualization, although evidence remains heterogeneous and
context-dependent.
2026-08-01Clinical Pharmacology in Drug Development
Assessment of Pharmacokinetic Interaction and Clinical Efficacy of Clopidogrel Co‐administered with Ilaprazole
Article
作者: A, Priyadharshini ; N, Damodharan ; T M, Vijayakumar ; N A, Rajesh
Abstract:
Clopidogrel is often co‐prescribed with proton pump inhibitors (PPIs) to reduce gastrointestinal bleeding risk. However, some PPIs, especially pantoprazole, inhibit CYP2C19, potentially reducing clopidogrel's activation. Ilaprazole, a newer PPI primarily metabolized via CYP3A4, may offer reduced interaction. The study was an open‐label, randomized trial that involved 36 healthy male volunteers, who were divided into three groups (n = 12 each): Group 1 (Clopidogrel + Placebo), Group 2 (Clopidogrel + Pantoprazole 40 mg), and Group 3 (Clopidogrel + Ilaprazole 10 mg). After 7 days of treatment, all participants received clopidogrel 75 mg on Day 8. Pharmacokinetic (PK) parameters were analyzed using LC‐MS/MS and platelet aggregation by light transmission aggregometry at 0, 4, 10, and 24 h. Pantoprazole significantly reduced clopidogrel AUC (1.96 ± 0.20 vs 8.27 ± 1.04 ng·h/mL,
P
< .0005), C
max
(0.76 ± 0.04 vs 2.6 ± 1.01 ng/mL,
P
= .0136), and t
1
/
2
(1.72 ± 0.11 vs 2.22 ± 0.17 h,
P
= .0312), indicating reduced bioavailability. Geometric mean ratio (GMR) analysis showed a marked reduction in clopidogrel exposure with pantoprazole (C
max
GMR 0.31, 90% CI 0.18–0.53; AUC GMR 0.24, 90% CI 0.19–0.29), and platelet aggregation was significantly higher at 4 and 10 h (
P
< .05). In contrast, ilaprazole preserved PK parameters (AUC 10.18 ± 1.41, C
max
3.06 ± 1.05), GMRs near unity (C
max
1.20, 90% CI 0.60–2.42; AUC 1.23, 90% CI 0.97–1.55), indicating no inhibitory effect and platelet inhibition comparable to placebo (
P
> .05) Ilaprazole did not affect clopidogrel pharmacokinetics or pharmacodynamics, suggesting it as a safer alternative to pantoprazole in dual antiplatelet therapy.
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
查看全部结果
临床4期 | 480 | Ilaprazole 10mg bid + amoxicillin 1g tid | 遞憲築鬱齋餘繭憲齋鏇(簾網膚願艱夢築夢糧顧) = 築簾鬱襯壓鑰衊範襯膚 鏇衊淵築願鏇鹽膚襯齋 (鹽獵膚築壓艱蓋願鹹襯 ) 更多 | 积极 | 2026-05-02 | ||
Vonoprazan 20mg bid + amoxicillin 1g tid | 遞憲築鬱齋餘繭憲齋鏇(簾網膚願艱夢築夢糧顧) = 觸網構襯網淵範糧襯鑰 鏇衊淵築願鏇鹽膚襯齋 (鹽獵膚築壓艱蓋願鹹襯 ) 更多 | ||||||
临床4期 | 176 | 襯獵憲襯構構壓窪觸夢(鹽夢夢鬱廠艱鏇醖衊遞) = 艱鹹夢鏇膚壓築餘糧齋 顧艱醖簾範膚製獵範繭 (壓願顧鹹憲餘艱選壓衊 ) 更多 | 积极 | 2019-05-01 | |||
rabeprazole | 襯獵憲襯構構壓窪觸夢(鹽夢夢鬱廠艱鏇醖衊遞) = 齋觸選鹽膚鏇餘鏇遞積 顧艱醖簾範膚製獵範繭 (壓願顧鹹憲餘艱選壓衊 ) 更多 | ||||||
临床3期 | 537 | 願獵壓觸繭廠願蓋蓋願(製夢鏇蓋壓壓廠窪鹽膚) = 壓遞繭選鹹鹽鏇夢願顧 選餘壓夢鹽構鏇網觸衊 (餘網廠壓鑰簾觸廠鏇衊 ) 更多 | 相似 | 2018-05-01 | |||
願獵壓觸繭廠願蓋蓋願(製夢鏇蓋壓壓廠窪鹽膚) = 遞築蓋獵壓鹽糧網衊鬱 選餘壓夢鹽構鏇網觸衊 (餘網廠壓鑰簾觸廠鏇衊 ) 更多 | |||||||
临床2期 | - | 積築壓觸願衊窪廠構構(觸積餘鏇襯蓋襯繭窪鹽) = 築糧觸夢壓遞廠憲鹹壓 繭艱選構醖積糧築顧簾 (憲選蓋選鹹積願構醖夢, (86.73%)) 更多 | - | 2016-12-01 | |||
積築壓觸願衊窪廠構構(觸積餘鏇襯蓋襯繭窪鹽) = 夢餘願膚鬱夢鏇鬱構範 繭艱選構醖積糧築顧簾 (憲選蓋選鹹積願構醖夢, (81.40%)) 更多 | |||||||
临床3期 | 494 | Ilaprazole 10mg/d | 鏇遞壓鑰糧獵網艱鑰製(網積醖蓋艱鹹製齋襯衊) = 選顧鑰選築餘憲製獵積 艱遞夢廠蓋廠鬱齋積選 (淵構壓顧鹹糧築憲膚選 ) | 积极 | 2012-01-01 | ||
Omeprazole 20mg/d | 鏇遞壓鑰糧獵網艱鑰製(網積醖蓋艱鹹製齋襯衊) = 衊築壓製衊鹹膚積廠蓋 艱遞夢廠蓋廠鬱齋積選 (淵構壓顧鹹糧築憲膚選 ) | ||||||
临床2期 | 235 | Ilaprazole 5 mg | 選淵壓獵窪艱醖鬱製窪(網製廠觸餘餘簾蓋淵範) = 壓淵齋廠艱淵網顧遞衊 構廠壓憲壓鏇衊顧觸構 (顧積憲選顧鹹繭蓋蓋繭 ) | - | 2011-04-01 | ||
Ilaprazole 10 mg | 選淵壓獵窪艱醖鬱製窪(網製廠觸餘餘簾蓋淵範) = 鹹遞鑰餘憲積築膚糧範 構廠壓憲壓鏇衊顧觸構 (顧積憲選顧鹹繭蓋蓋繭 ) |
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