预约演示
更新于：2025-02-05
Linaprazan glurate
戊二酸利那拉生酯
更新于：2025-02-05
概要
基本信息
原研机构 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 中国 (2024-12-01), |
最高研发阶段(中国)批准上市 |
特殊审评- |
登录后查看时间轴
结构/序列
分子式C26H32N4O5 |
InChIKeyGPHPBXRKAJSSIC-UHFFFAOYSA-N |
CAS号1228559-81-6 |
关联
8
项与 戊二酸利那拉生酯 相关的临床试验NCT05742984
Ph 1, OL, Randomized, Parallel-group Study to Investigate PK and PD (Intragastric pH) of Linaprazan Glurate/Linaprazan After 14 Days Administration of Linaprazan Glurate to Healthy Subjects
CTR20220258
[14C]X842在中国成年男性健康受试者体内的物质平衡与生物转化临床研究
NCT05055128
A Randomized Double-blind, Double Dummy, Active Comparator-controlled Dose-finding Study in Patients With Erosive Esophagitis Due to Gastro-esophageal Reflux Disease (GERD) Los Angeles Grade C or D, and Patients With at Least Partial Symptom Response But Endoscopically Still Unhealed After 8 Weeks History of Standard Treatment Healing Course With Proton-pump Inhibitor (PPI), to Investigate Safety, Tolerability, and Healing Rates After 4 Weeks Treatment of X842 or Lansoprazole, and Symptom Pattern During Subsequent 4 Weeks Treatment With Lansoprazole
100 项与 戊二酸利那拉生酯 相关的临床结果
登录后查看更多信息
100 项与 戊二酸利那拉生酯 相关的转化医学
登录后查看更多信息
100 项与 戊二酸利那拉生酯 相关的专利（医药）
登录后查看更多信息
3
项与 戊二酸利那拉生酯 相关的文献（医药）2025-01-21Clinical and Translational Gastroenterology
A Randomized, Comparative Trial of a Potassium-Competitive Acid Blocker (X842) and Lansoprazole for the Treatment of Patients with Erosive Esophagitis.
Article
作者: Li, Xing ; Meng, Fandong ; Zhang, Shutian ; Hu, Jiuye ; Han, Muzhou ; Shao, Dong ; Wu, Yongdong ; Xu, Baohong ; Liu, Xiaowei ; Zhang, Zhenyu ; Tuo, Biguang ; He, Song ; Tang, Haitao ; Zhen, Yanbo ; Wang, Shenglan ; Zhu, Siying ; Miu, Yangde ; Hu, Pingsheng ; Zong, Ye ; Liu, Qi ; Xiu, Jin ; Lu, Ming ; Wang, Qizhi ; Liu, Chengxia
INTRODUCTION:
X842 is a new type of gastric acid-suppressing agent with a rapid onset of action and a long duration of effect. We aim to investigate the efficacy and safety of different doses of X842 versus lansoprazole in the treatment of patients with erosive esophagitis (EE).
METHODS:
This phase 2 study included 90 patients with EE (Los Angeles grades A-D) who were randomized (1:1:1) to receive oral low-dose X842 (50 mg/day, n=31), high-dose X842 (100 mg/day, n=31), or lansoprazole (30 mg/day, n=30) for 4 weeks. The main efficacy endpoint was the EE healing rate, which was the proportion of patients who achieved endoscopic healing after 4 weeks of treatment.
RESULTS:
For ITT analysis, the EE healing rates at 4 weeks were 93.6% (29/31), 79.3% (23/29), and 80.0% (24/30) for the X842 50 mg, the X842 100 mg and the lansoprazole 30 mg groups. For PP analysis, the EE healing rates at 4 weeks were 93.6% (29/31), 80.8% (21/26), and 82.1% (23/28) in the three groups, respectively. The EE healing rate did not significantly differ among the three groups in either the ITT (p = 0.2351) or PP (p = 0.3320) analysis. The incidence of drug-related treatment-emergent adverse events (TEAEs) did not differ among groups. No severe drug-related TEAEs occurred in the X842 group.
CONCLUSIONS:
Our findings confirmed that X842 had efficacy and a favourable safety profile similar to those of lansoprazole. Therefore, X842, a novel P-CAB, is expected to become a promising therapeutic agent for EE.
2024-05-01Journal of pharmaceutical and biomedical analysis
Absorption, distribution, metabolism and excretion of linaprazan glurate in rats
Article
作者: Zhang, Xinyue ; Zheng, Yuandong ; Yuan, Yali ; Diao, Xingxing ; Yang, Ying ; Xiu, Jin ; Yang, Chen ; Lu, Ming ; Liu, Donghui ; Hu, Pingsheng
Linaprazan (AZD0865, TX07) is one of potassium-competitive acid blockers. However, linaprazan is rapidly excreted from the body, shortening its acid inhibition property. Linaprazan glurate (X842) is a prodrug of linaprazan with a prolonged inhibitory effect on gastric acid secretion. Linaprazan glurate has entered clinical trials, but few studies have reported its metabolism in non-clinical and clinical settings. In this study, we studied the pharmacokinetics, tissue distribution, mass balance, and metabolism of linaprazan glurate in rats after a single oral dose of 2.4 mg/kg (100 µCi/kg) [14C]linaprazan glurate. The results demonstrated that linaprazan glurate was mainly excreted via feces in rats with 70.48% of the dose over 168 h. The plasma AUC0-∞ of linaprazan glurate in female rats was 2 times higher than that in male rats. Drug-related substances were mainly concentrated in the stomach, eyes, liver, small intestine, and large intestine after administration. In blood, drug-related substances were mostly distributed into plasma instead of hemocytes. In total, 13 metabolites were detected in rat plasma, urine, feces, and bile. M150 (2,6-dimethylbenzoic acid) was the predominant metabolite in plasma, accounting for 80.65% and 67.65% of AUC0-24h in male and female rats, respectively. Based on the structures, linaprazan glurate was mainly hydrolyzed into linaprazan, followed by a series of oxidation, dehydrogenation, and glucuronidation in rats. Besides, CES2 is the main metabolic enzyme involved in the hydrolysis of linaprazan glurate to linaprazan.
2023-02-01Archives of microbiology
Formulation-based antagonistic endophyte Amycolatopsis sp. SND-1 triggers defense response in Vigna radiata (L.) R. Wilczek. (Mung bean) against Cercospora leaf spot disease
Article
作者: Kumar, Raju Suresh ; Nayaka, Sreenivasa ; Basavarajappa, Dhanyakumara Shivapoojar
In the present work, Amycolatopsis sp. SND-1 (SND-1) was isolated from Cleome chellidonii Linn. (C. chellidonii) was performed as biocontrol and resistance elicitor in Vigna radiata (L.) R. Wilczek (mung bean) plants against Cercospora leaf spot causing pathogen Cercospora canescens (C. canescens). The SND-1 isolate showed 74% of inhibition against C. canescens in dual culture and GC-MS analysis revealed the presence of antifungal compounds. Molecular characterization through 16S rRNA showed that the isolated SND-1 belongs to Amycolatopsis sp. The in vitro plant growth trials exhibited production of indole acetic acid, gibberellic acid, cytokinin, ammonia, hydrogen cyanide, and siderophore and phosphate solubilization. In vivo study with talcum formulation of SND-1 revealed a significant increase in plant root length, shoots length, root and shoot fresh weight, and reduced the disease severity in treated mung bean plants. Triggering of resistance by SND-1 formulation was studied by histochemical depositions and biochemical defense enzymes that resulted in the acceleration in defense response in comparison with control plants. The bioactive endophytic Amycolatopsis sp. SND-1 enhanced the defense against C. canescens infection; hence, it can be used as a biological control agent in mung bean cultivars.
100 项与 戊二酸利那拉生酯 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 反流性食管炎 | 中国 | 2024-12-01 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 糜烂性食管炎 | 临床2期 | 美国 | 2021-08-11 | |
| 糜烂性食管炎 | 临床2期 | 保加利亚 | 2021-08-11 | |
| 糜烂性食管炎 | 临床2期 | 捷克 | 2021-08-11 | |
| 糜烂性食管炎 | 临床2期 | 格鲁吉亚 | 2021-08-11 | |
| 糜烂性食管炎 | 临床2期 | 匈牙利 | 2021-08-11 | |
| 糜烂性食管炎 | 临床2期 | 波兰 | 2021-08-11 | |
| 糜烂性食管炎 | 临床2期 | 塞尔维亚 | 2021-08-11 | |
| 糜烂性食管炎 | 临床2期 | 乌克兰 | 2021-08-11 | |
| 胃食管反流 | 临床2期 | 欧盟 | 2020-01-22 | |
| 十二指肠溃疡 | 临床2期 | 中国 | - |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | - | - | 餘蓋顧築範鹹選積廠觸(觸蓋鏇築鹹製遞觸醖齋): RR = 1.17 (95% CI, 1.11 ~ 1.22) | - | 2024-05-18 | ||
Conventional PPI-based triple therapy | |||||||
临床2期 | 248 | (X842 25 mg BID) | 製鹽憲觸憲夢蓋積糧醖(襯餘觸製網淵壓淵齋製) = 積鏇築選壓鹹淵遞憲憲 憲選糧觸獵鏇選鑰夢遞 (簾網膚憲餘繭範願獵齋, 餘顧衊鏇選淵窪築餘醖 ~ 窪構艱糧窪積製獵餘鑰) 更多 | - | 2023-11-01 | ||
(X842 50 mg BID) | 製鹽憲觸憲夢蓋積糧醖(襯餘觸製網淵壓淵齋製) = 簾鏇醖夢窪鏇製艱淵艱 憲選糧觸獵鏇選鑰夢遞 (簾網膚憲餘繭範願獵齋, 窪窪艱網遞壓鏇繭襯構 ~ 願醖膚遞齋夢鬱獵餘醖) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
来和芽仔聊天吧
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用