预约演示
更新于：2026-01-27
Lafutidine
拉呋替丁
更新于：2026-01-27
概要
基本信息
原研机构 |
权益机构- |
最高研发阶段批准上市 |
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C22H29N3O4S |
InChIKeyKMZQAVXSMUKBPD-DJWKRKHSSA-N |
CAS号206449-93-6 |
关联
26
项与 拉呋替丁 相关的临床试验CTR20251518
拉呋替丁片（10 mg）随机、开放、两周期、两交叉单次给药空腹/餐后状态下在健康受试者中的生物等效性试验
CTR20221286
拉呋替丁片随机、开放、两制剂、双周期、双交叉、空腹及餐后单次给药后健康人体生物等效性试验
ChiCTR2200055479
Efficacy of nocturnal symptoms and esophageal acid exposure in GERD patients: a randomized controlled study of PPI combined with lafutidine versus PPI alone
100 项与 拉呋替丁 相关的临床结果
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100 项与 拉呋替丁 相关的转化医学
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100 项与 拉呋替丁 相关的专利（医药）
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157
项与 拉呋替丁 相关的文献（医药）2024-11-01Annals of Palliative Medicine
Assessing lafutidine’s potential to protect lung cancer patients from chemotherapy-induced neuropathy
Article
作者: Khan, Saim Mahmood ; Hussain, Jawairya Muhammad ; Sultan, Ramsha
2024-09-01EBioMedicine
Tanomastat exerts multi-targeted inhibitory effects on viral capsid dissociation and RNA replication in human enteroviruses
Article
作者: Yogarajah, Thinesshwary ; Chu, Justin Jang Hann ; Jaladanki, Chaitanya K. ; Lim, Therese Yien May ; Fan, Hao ; Wong, Yi Hao ; Jaladanki, Chaitanya K
BACKGROUND:
Global cyclical outbreaks of human enterovirus infections has positioned human enterovirus A71 (EV-A71) as a neurotropic virus of clinical importance. However, there remains a scarcity of internationally approved antivirals and vaccines.
METHODS:
In pursuit of repurposing drugs for combating human enteroviruses, we employed a comprehensive pharmacophore- and molecular docking-based virtual screen targeting EV-A71 capsid protein VP1-4, 3C protease, and 3D polymerase proteins. Among 15 shortlisted ligand candidates, we dissected the inhibitory mechanism of Tanomastat in cell-based studies and evaluated its in vivo efficacy in an EV-A71-infected murine model.
FINDINGS:
We demonstrated that Tanomastat exerts dose-dependent inhibition on EV-A71 replication, with comparable efficacy profiles in enterovirus species A, B, C, and D in vitro. Time-course studies suggested that Tanomastat predominantly disrupts early process(es) of the EV-A71 replication cycle. Mechanistically, live virus particle tracking and docking predictions revealed that Tanomastat specifically impedes viral capsid dissociation, potentially via VP1 hydrophobic pocket binding. Bypassing its inhibition on entry stages, we utilized EV-A71 replication-competent, 3Dpol replication-defective, and bicistronic IRES reporter replicons to show that Tanomastat also inhibits viral RNA replication, but not viral IRES translation. We further showed that orally administered Tanomastat achieved 85% protective therapeutic effect and alleviated clinical symptoms in EV-A71-infected neonatal mice.
INTERPRETATION:
Our study establishes Tanomastat as a broad-spectrum anti-enterovirus candidate with promising pre-clinical efficacy, warranting further testing for potential therapeutic application.
FUNDING:
MOE Tier 2 grants (MOE-T2EP30221-0005, R571-000-068-592, R571-000-076-515, R571-000-074-733) and A∗STARBiomedical Research Council (BMRC).
2024-05-01BIOMEDICINE & PHARMACOTHERAPY
Utilizing machine learning to identify nifuroxazide as an inhibitor of ubiquitin-specific protease 21 in a drug repositioning strategy
Article
作者: Nguyen, Tan Khanh ; Lee, Kyeong ; Ahn, Hee-Chul ; Kim, Sang Geon ; Tak, Jihoon
Ubiquitin-specific protease (USP), an enzyme catalyzing protein deubiquitination, is involved in biological processes related to metabolic disorders and cancer proliferation. We focused on constructing predictive models tailored to unveil compounds boasting USP21 inhibitory attributes. Six models, Extra Trees Classifier, Random Forest Classifier, LightGBM Classifier, XGBoost Classifier, Bagging Classifier, and a convolutional neural network harnessed from empirical data were selected for the screening process. These models guided our selection of 26 compounds from the FDA-approved drug library for further evaluation. Notably, nifuroxazide emerged as the most potent inhibitor, with a half-maximal inhibitory concentration of 14.9 ± 1.63 μM. The stability of protein-ligand complexes was confirmed using molecular modeling. Furthermore, nifuroxazide treatment of HepG2 cells not only inhibited USP21 and its established substrate ACLY but also elevated p-AMPKα, a downstream functional target of USP21. Intriguingly, we unveiled the previously unknown capacity of nifuroxazide to increase the levels of miR-4458, which was identified as downregulating USP21. This discovery was substantiated by manipulating miR-4458 levels in HepG2 cells, resulting in corresponding changes in USP21 protein levels in line with its predicted interaction with ACLY. Lastly, we confirmed the in vivo efficacy of nifuroxazide in inhibiting USP21 in mice livers, observing concurrent alterations in ACLY and p-AMPKα levels. Collectively, our study establishes nifuroxazide as a promising USP21 inhibitor with potential implications for addressing metabolic disorders and cancer proliferation. This multidimensional investigation sheds light on the intricate regulatory mechanisms involving USP21 and its downstream effects, paving the way for further exploration and therapeutic development.
100 项与 拉呋替丁 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 | 日本 | 2014-10-07 | |
| 胃炎 | 日本 | 2000-04-06 | |
| 消化性溃疡 | 日本 | - | 2000-01-18 |
| 十二指肠溃疡 | 日本 | 2000-01-08 | |
| 胃食管反流 | 日本 | 2000-01-08 | |
| 胃溃疡 | 日本 | 2000-01-08 |
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 |
|---|---|---|---|---|
| 糜烂性食管炎 | 临床3期 | - | 2011-11-01 | |
| 炎症性肠病 | 临床前 | 日本 | - | - |
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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3期 | 495 | (Lafutidine) | 齋獵觸觸選齋鬱顧壓構: P-Value = 0.05 更多 | - | 2020-09-16 | ||
(Famotidine) | |||||||
N/A | 胃癌 辅助 | - | 窪鑰鏇獵夢築簾鬱選獵(憲壓淵襯襯淵鑰構繭簾) = 窪醖餘糧願廠壓鬱簾選 獵網蓋鹽鹽膚築夢積艱 (製鏇衊衊繭醖範遞淵艱 ) 更多 | 积极 | 2018-02-26 | ||
窪鑰鏇獵夢築簾鬱選獵(憲壓淵襯襯淵鑰構繭簾) = 選範鏇艱範鬱艱遞糧壓 獵網蓋鹽鹽膚築夢積艱 (製鏇衊衊繭醖範遞淵艱 ) 更多 | |||||||
临床3期 | - | 願夢衊鹽鹹鑰廠鑰憲鑰(襯蓋膚網膚艱遞遞鬱簾) = 鏇壓糧獵選餘鑰觸壓鬱 繭衊構餘繭鏇願糧廠遞 (獵淵醖鏇網顧製鬱積夢 ) 更多 | - | 2010-04-01 | |||
願夢衊鹽鹹鑰廠鑰憲鑰(襯蓋膚網膚艱遞遞鬱簾) = 構淵餘繭觸範餘壓艱簾 繭衊構餘繭鏇願糧廠遞 (獵淵醖鏇網顧製鬱積夢 ) |
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