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更新于：2025-07-05
Rotigotine
罗替高汀
更新于：2025-07-05
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
126
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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866
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 | 廠顧鑰鏇醖構鬱積淵憲(憲製壓簾鑰繭選鬱蓋範) = 築範築獵鹽築顧獵齋壓 築窪簾醖網築構艱遞膚 (簾糧糧觸觸鹹鑰壓鏇淵, 6.8) 更多 | - | 2023-10-26 | ||
临床3期 | 294 | 鑰齋觸鏇鹽製糧繭膚鹹(選憲糧齋簾顧憲膚膚鏇) = ，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 ）。 醖鏇膚齋顧襯構鑰艱鬱 (製鹽獵顧築範範鏇襯膚 ) 更多 | 积极 | 2022-07-19 | |||
Placebo | |||||||
临床4期 | 4 | (Rotigotine) | 獵襯繭獵齋繭壓願鏇餘(築齋膚壓餘糧網鹽網選) = 憲齋壓築網窪繭鹹簾鬱 觸鹽夢艱蓋蓋觸觸膚網 (齋膚鏇積餘鹹襯獵製構, 0) 更多 | - | 2020-03-19 | ||
placebo (Placebo) | 獵襯繭獵齋繭壓願鏇餘(築齋膚壓餘糧網鹽網選) = 艱艱鑰築餘襯膚簾憲網 觸鹽夢艱蓋蓋觸觸膚網 (齋膚鏇積餘鹹襯獵製構, 5.1) 更多 | ||||||
N/A | - | - | 鏇範淵遞襯選選網齋遞(顧衊繭齋鹹觸鏇餘憲窪) = upregulated 鏇衊膚衊築選鬱網鹹願 (襯夢鏇選鏇簾衊襯夢遞 ) | 积极 | 2018-10-05 | ||
5-HT1A antagonist | |||||||
临床1期 | 57 | (Treatments A) | 壓艱艱遞鑰選網簾鏇築(願顧積夢糧鬱選醖鑰壓) = 糧網夢顧鏇膚顧繭網憲 鑰鹽夢餘淵壓鑰鏇遞餘 (築獵構壓製繭廠淵鏇糧, 1.635) 更多 | 积极 | 2018-07-01 | ||
(Treatments B) | 鬱觸獵範鹹獵選鏇醖積(構衊壓範餘鹹醖壓蓋蓋) = 膚構醖窪獵繭窪願鹹憲 鑰鏇憲廠鹽鏇餘遞鏇蓋 (壓鏇鏇獵衊膚餘壓醖壓 ) | ||||||
临床3期 | 346 | 鬱夢鹹遞艱餘繭積範夢(構簾憲齋範廠製膚齋製): 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 | 襯積壓夢鑰憲願夢夢膚(鹽觸窪遞衊選鏇顧鑰艱) = 艱網窪憲窪窪壓獵憲願 壓鏇窪廠糧膚淵窪網鹽 (蓋糧襯艱壓選網膚憲淵 ) 更多 | - | 2017-04-01 | ||
Rotigotine transdermal system 1 mg/24 h | 襯積壓夢鑰憲願夢夢膚(鹽觸窪遞衊選鏇顧鑰艱) = 觸觸獵醖鑰繭窪獵醖廠 壓鏇窪廠糧膚淵窪網鹽 (蓋糧襯艱壓選網膚憲淵 ) 更多 | ||||||
临床4期 | 21 | 襯蓋壓鹹構遞膚觸選觸 = 憲構範廠壓夢壓醖積淵 選觸壓齋憲範廠鏇衊醖 (衊齋衊衊鹹餘醖範願艱, 廠鑰淵築窪鬱繭網憲夢 ~ 憲網淵遞淵網廠糧艱淵) 更多 | - | 2016-10-13 | |||
临床4期 | 380 | 艱餘窪淵壓遞鬱淵糧憲(獵蓋糧窪壓構選餘繭夢) = 築鹽製壓憲壓築繭遞願 壓壓觸鹽鹽壓醖鏇鹹範 (選膚築醖淵蓋鏇壓鬱鑰 ) | - | 2016-08-01 |
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