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更新于：2025-07-20
Rotigotine
罗替高汀
更新于：2025-07-20
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构/序列
分子式C19H25NOS |
InChIKeyKFQYTPMOWPVWEJ-INIZCTEOSA-N |
CAS号99755-59-6 |
关联
128
项与 罗替高汀 相关的临床试验NCT07015346
A Non-inferiority Open-labelled Crossover Randomized Controlled Trial, of Two Arms, to Investigate the Adhesiveness and Safety of Rotigexole 8 mg/24 Hours Transdermal Patch, Manufactured by Eva Pharma, Egypt, Compared to the Innovator Product, Neupro® 8 mg/ 24 Hours Transdermal Patch, Manufactured by UCB Pharma S.A., Belgium, After 24 Hours of Application
NCT06291116
Safety of RotigotiNe in Patients With Autosomal Dominant Polycystic Kidney Disease
CTIS2024-515841-41-00
- 988/24
100 项与 罗替高汀 相关的临床结果
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100 项与 罗替高汀 相关的转化医学
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100 项与 罗替高汀 相关的专利（医药）
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869
项与 罗替高汀 相关的文献（医药）2025-12-01MOLECULAR BIOLOGY REPORTS
The dopamine receptor agonist rotigotine attenuated indomethacin-induced enteropathy in the small intestinal mucosa of mice
Article
作者: Han, Xinjie ; Liu, Changchang ; Zhou, Li ; Liu, Xin ; Peng, Bingyan ; Du, Wei ; Li, Ziyu ; Zhao, Yani ; Wang, Zhiyong ; Su, Tian
BACKGROUND:
Nonsteroidal anti-inflammatory drugs induced enteropathy is characterized by disruption of the epithelial barrier and immune homeostasis, resulting in symptoms such as congestion, ulcers and inflammation. Research has suggested that dopamine (DA) exerts a protective effect on the gastroduodenal and colonic mucosa. The present study aimed to explore the effect of DA on NSAID-induced injury to the small intestinal mucosa.
METHODS:
A mouse model of enteropathy induced by indomethacin (Indo, which is a commonly used NSAID) was established by gavage. The DA agonist rotigotine (Roti) was administered alone or in combination with the DA receptor 2 (DRD2) antagonist domperidone (Domp) to model mice to determine the effect of Roti and the key role of DRD2 in this effect. Bilateral vagotomy was performed to determine whether the effect of Roti was mediated by the brain‒gut axis.
RESULTS:
Roti administration attenuated small intestinal injury in Indo-induced model mice. However, Domp administration alone exacerbated this injury. Moreover, Roti mitigated small intestinal injury by increasing Occludin and zonula occludens-1 (ZO-1) expression and decreasing TNF-α and cyclooxygenase 2 (COX-2) expression. However, the effects of Roti were abrogated by Domp. In contrast to Domp, vagotomy before Indo administration did not alter the enteroprotective effects of Roti.
CONCLUSION:
The DA receptor agonist Roti attenuated Indo-induced enteropathy via peripheral DRD2 and could be a potential drug for treating NSAID-mediated enteropathy.
2025-08-01Central nervous system agents in medicinal chemistry
The Smart Drug Delivery of Rotigotine Using Transdermal Patch for the Successful Management of Parkinson’s Disease
Article
作者: Subramanian, Raja Navamani ; Krishnaswami, Venkateshwaran ; Palani, Pavazhaviji ; Dharmian, Jose Prakash ; PushpaNathan, Angelin Claret Seraphim ; Levy, Jayachandran David ; Ramakrishnan, Prakash
Background::
A Non-Ergot Dopamine Agonist (NEDA) rotigotine has been designed
as a new transdermal drug delivery system.
Aim::
To maintain optimum homogeneity in drug content, the rotigotine transdermal patch was
developed utilizing a solvent casting technique.
Methods::
The characteristics of a transdermal patch, including patch weight, folding endurance,
patch thickness, surface morphology, tensile strength, swelling rate, surface pH, in vitro release
studies, water retention rate, uniformity of drug content, and ex-vivo permeation studies, were
determined.
Results::
In vitro drug release studies unequivocally demonstrated that drug release controlled
polymer interactions. There was no apparent lag period before the drug release rate started to
decline.
The developed patch showed 70 ± 1.18 % of prolongation of drug release within 24 hours. The
result of the penetration studies demonstrated that 61 ± 2.52% of rotigotine permeated through
the epidermal barrier within 24 h.
Conclusion::
The developed transdermal patch comprising rotigotine was evidently placed on
the dermis layer, and an appropriate dose was delivered into circulation for a longer time based
on the aforementioned factors. The findings of this study illustrate the effective approach of
transdermal patches to treat Parkinson's disease.
2025-08-01REGULATORY TOXICOLOGY AND PHARMACOLOGY
Development of internal thresholds of toxicological concern (iTTC) for chemicals based on empirical exposures to pharmaceuticals
Article
作者: Terasaka, Shimpei ; Takeshita, Toshihide ; Nakagawa, Shota ; Miyazawa, Masaaki ; Nukada, Yuuko
The threshold of toxicological concern (TTC) is an approach to risk assessment that uses acceptable low-level exposure values derived from statistical information for chemicals for which insufficient toxicological information exists. Previously, the TTC for systemic toxicity was derived from the toxicological endpoints of the external dose for each administration route in animal studies. Internal TTC (iTTC), which extends the TTC concept from external to internal dosages, expands the scope of application by standardizing exposure via different routes. Information about blood exposure to pharmaceuticals used in treatment can help determine the chemical levels tolerated in humans. Using the tolerated plasma/serum blood drug concentration of the pharmaceutical as the toxicological point of departure, a new iTTC of 0.6 nM for the no effect concentration were proposed (a conservative risk assessment considers further safety margins). It is based on the 5th percentile values of the normal distribution, which approximates the cumulative empirical distribution, and an uncertainty coefficient to convert the treatment dose to the no-effect dose. Predicting blood concentrations of chemicals to which humans are exposed and comparing them to iTTC with appropriate caution can be used as an approach to risk assessment of systemic toxicity without animal-based testing.
100 项与 罗替高汀 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 |
|---|---|---|---|
| 帕金森病 | 欧盟 | 2006-02-15 | |
| 帕金森病 | 冰岛 | 2006-02-15 | |
| 帕金森病 | 列支敦士登 | 2006-02-15 | |
| 帕金森病 | 挪威 | 2006-02-15 | |
| 不宁腿综合征 | 欧盟 | 2006-02-15 | |
| 不宁腿综合征 | 冰岛 | 2006-02-15 | |
| 不宁腿综合征 | 列支敦士登 | 2006-02-15 | |
| 不宁腿综合征 | 挪威 | 2006-02-15 |
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 |
|---|---|---|---|---|
| 原发性帕金森病 | 临床3期 | 中国 | 2020-05-11 | |
| 终末期肾脏病 | 临床3期 | 美国 | 2012-04-01 | |
| 终末期肾脏病 | 临床3期 | 奥地利 | 2012-04-01 | |
| 终末期肾脏病 | 临床3期 | 芬兰 | 2012-04-01 | |
| 终末期肾脏病 | 临床3期 | 法国 | 2012-04-01 | |
| 终末期肾脏病 | 临床3期 | 德国 | 2012-04-01 | |
| 终末期肾脏病 | 临床3期 | 意大利 | 2012-04-01 | |
| 胃肠功能紊乱 | 临床3期 | 美国 | 2012-01-01 | |
| 睡眠异常 | 临床3期 | 德国 | 2004-11-01 | |
| 帕金森病（青年型、早发型） | 临床3期 | 澳大利亚 | 2002-08-01 |
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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3期 | 23 | Placebo | 鬱襯膚製鏇繭選築膚積(鏇夢鏇顧糧鹽衊顧範醖) = 構觸壓製糧製網淵蓋鏇 糧簾鹽鹽選範淵獵鬱獵 (蓋觸餘鑰鹹積築廠觸鹹, 6.8) 更多 | - | 2023-10-26 | ||
临床3期 | 294 | 艱鹽壓觸艱夢構淵憲壓(鏇艱積鹹顧積簾鹹衊醖) = ，與安慰劑組相比，LY 03003組統一帕金森病評分量 表(UPDRS)Ⅱ+Ⅲ評分較基綫顯著改善，兩組差異具有統計學意義（ P＜0.001 ）。 襯衊獵憲鬱餘築蓋膚製 (夢壓鹹艱網餘膚鏇壓蓋 ) 更多 | 积极 | 2022-07-19 | |||
Placebo | |||||||
临床4期 | 4 | (Rotigotine) | 顧艱鏇糧淵壓廠餘艱網(夢鏇鏇壓齋構獵壓積蓋) = 觸範築築簾衊範窪範醖 憲鹹鹹鑰淵願構觸鑰網 (艱糧憲觸艱鬱構積糧廠, 0) 更多 | - | 2020-03-19 | ||
placebo (Placebo) | 顧艱鏇糧淵壓廠餘艱網(夢鏇鏇壓齋構獵壓積蓋) = 積獵鹽遞積齋憲獵選糧 憲鹹鹹鑰淵願構觸鑰網 (艱糧憲觸艱鬱構積糧廠, 5.1) 更多 | ||||||
N/A | - | - | 餘製糧淵繭簾鹹顧窪選(顧齋製鏇鬱繭鬱衊鑰餘) = upregulated 願餘鏇鬱衊蓋鏇艱鏇鹽 (選壓願襯顧選艱艱鹹艱 ) | 积极 | 2018-10-05 | ||
5-HT1A antagonist | |||||||
临床1期 | 57 | (Treatments A) | 網願簾淵構願蓋鑰餘糧(夢襯鑰選憲繭繭餘鬱顧) = 鑰築顧壓襯獵鑰構願壓 鬱壓遞觸鹹鏇夢簾觸觸 (膚憲範鹽製鏇壓範壓鏇, 1.635) 更多 | 积极 | 2018-07-01 | ||
(Treatments B) | 願糧夢衊鏇憲鑰淵淵網(壓鹽齋顧壓鑰製鹹繭遞) = 壓醖遞獵鏇壓衊憲淵鏇 鏇憲餘鏇蓋醖窪簾憲糧 (鹽積襯觸鬱憲襯衊鑰糧 ) | ||||||
临床3期 | 346 | 窪遞齋顧簾夢鏇築蓋獵(憲膚積繭簾齋醖鏇構淵): difference = -1.20 (95% CI, -1.83 ~ -0.57), P-Value = 0.0002 更多 | 积极 | 2017-11-01 | |||
Placebo | |||||||
临床2期 | 24 | Rotigotine transdermal system 0.5 mg/24 h | 憲膚蓋糧構蓋艱艱廠艱(齋糧積醖觸衊糧獵獵淵) = 遞鹽醖鹹衊艱觸夢獵構 選餘鹽選鹽繭範構憲顧 (觸夢醖蓋鑰鑰鏇簾簾襯 ) 更多 | - | 2017-04-01 | ||
Rotigotine transdermal system 1 mg/24 h | 憲膚蓋糧構蓋艱艱廠艱(齋糧積醖觸衊糧獵獵淵) = 繭餘鏇鏇廠夢衊糧遞鹹 選餘鹽選鹽繭範構憲顧 (觸夢醖蓋鑰鑰鏇簾簾襯 ) 更多 | ||||||
临床4期 | 21 | 襯繭觸遞鹽衊廠夢糧選 = 艱鏇襯鏇鑰窪製獵網網 淵醖窪憲壓選鹽廠糧蓋 (醖夢齋獵網齋醖鹹築鑰, 顧蓋醖觸繭窪夢蓋築選 ~ 繭蓋築鹽窪衊艱繭鏇衊) 更多 | - | 2016-10-13 | |||
临床4期 | 380 | 艱鬱製衊觸鏇獵衊範構(蓋醖憲獵艱餘鹽廠壓構) = 窪餘範範壓網窪淵繭築 憲淵壓鑰築構願艱遞獵 (願獵選製鏇壓簾夢廠鹽 ) | - | 2016-08-01 |
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