预约演示
更新于：2025-07-31
Carbidopa/Entacapone/Levodopa
卡比多巴/恩他卡朋/左旋多巴
更新于：2025-07-31
概要
基本信息
药物类型 小分子化药 |
别名 Levodopa/Carbidopa Hydrate/Entacapone、Levodopa/Carbidopa/Entacapone、恩他卡朋双多巴 + [9] |
作用方式 抑制剂、拮抗剂 |
作用机制 COMT抑制剂(儿茶酚氧位甲基转移酶抑制剂)、DDC抑制剂(DOPA脱羧酶抑制剂)、DRDs拮抗剂(多巴胺受体家族拮抗剂) |
在研适应症 |
非在研适应症- |
非在研机构- |
权益机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2003-06-11), |
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C33H40N6O13 |
InChIKeyOTVUCEMFRGJEMR-FTXVUGNJSA-N |
CAS号745835-09-0 |
关联
44
项与 卡比多巴/恩他卡朋/左旋多巴 相关的临床试验CTR20244200
恩他卡朋双多巴片（Ⅱ）在健康受试者中随机、开放、两制剂、四周期、完全重复交叉设计、餐后状态下的生物等效性试验
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恩他卡朋双多巴片（Ⅱ）人体生物等效性研究
CTR20244199
恩他卡朋双多巴片（Ⅱ）在健康受试者中随机、开放、两制剂、四周期、完全重复交叉设计、空腹状态下的生物等效性试验
100 项与 卡比多巴/恩他卡朋/左旋多巴 相关的临床结果
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100 项与 卡比多巴/恩他卡朋/左旋多巴 相关的转化医学
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100 项与 卡比多巴/恩他卡朋/左旋多巴 相关的专利（医药）
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84
项与 卡比多巴/恩他卡朋/左旋多巴 相关的文献（医药）2024-08-01Neurology and Therapy
The Catechol O-Methyltransferase Inhibitor Entacapone in the Treatment of Parkinson’s Disease: Personal Reflections on a First-in-Class Drug Development Programme 40 Years On
Review
作者: Pollesello, Piero ; Männistö, Pekka T ; Hanttu, Anna ; Keränen, Tapani ; Reinikainen, Kari J
In the 1980s, Orion Pharma, then a mid-ranking Nordic area pharmaceutical company, established a drug development programme on the inhibition of catechol O-methyltransferase (COMT). This enzyme, which plays an important role in the inactivation of catecholamine neurotransmitters and drugs with a catechol structure, thus came under consideration as a target in the innovative translational and clinical programme we describe in this historical review. The starting point was the conjecture that a peripherally acting COMT inhibitor might improve entry of levodopa into the brain. This had potentially significant implications for the medical treatment of Parkinson's disease (PD). The rationale was that more efficient delivery of levodopa to the brain might allow the high therapeutic doses of levodopa to be reduced and the dose interval to be extended. Elucidation of structure-activity relations paved the way for the discovery and development of entacapone, a 5-nitrocatechol that was a potent and highly specific inhibitor of COMT. Experience in phase III clinical trials established that entacapone, used as an adjunct to regular or controlled-release levodopa preparations (also including a peripherally acting dopa-decarboxylase inhibitor), increased ON-time and reduced OFF-time and improved clinical condition in patients with PD experiencing wearing-off, often with a reduced daily levodopa dose. Several of these studies also identified that entacapone improved patients' quality of life and was cost-effective. Subsequently, entacapone has been amalgamated into a triple-combination preparation (Stalevo®) with levodopa and carbidopa to create a flexible and convenient drug therapy for patients with PD who have end-of-dose motor fluctuations not stabilised on levodopa/dopa-decarboxylase inhibitor treatment. This review offers a historical perspective on a successful programme of drug development by researchers who played central roles in the progress from exploratory hypothesis to registered pharmaceutical product.
2023-11-01European journal of neurology
Real-world considerations regarding the use of the combination of levodopa, carbidopa, and entacapone (Stalevo® ) in Parkinson's disease.
Review
作者: Reichmann, Heinz
An important aim in long-term levodopa therapy is to prolong the duration of symptomatic efficacy of each dose without increasing peak plasma concentrations above the threshold for the emergence of dyskinesias. One strategy is to enhance levodopa delivery to the brain by co-administering it with inhibitors of peripheral dopa-decarboxylase and catechol-O-methyltransferase (COMT). Levodopa, carbidopa and entacapone (LCE), available in a range of fixed-dose combinations as the branded formulation Stalevo® (Orion Pharma), has been developed to address this requirement and has been in general use for 20 years, having first been evaluated in randomized controlled trials. Experience with LCE has established that improved levodopa pharmacokinetics achieved with dual-enzyme inhibition are translated into improved clinical efficacy, including the possibility of reducing total levodopa dosage with no loss of therapeutic effect. The ease and tolerability of switching to LCE has been affirmed in the SIMCOM trial and by personal experience detailed in this review. Some 300,000 patient-years of safety data are available for LCE, including trial data for up to 5 years. Most adverse effects associated with LCE are attributable to the levodopa component rather than the enzyme inhibitors. The hepatotoxicity observed with the class comparator tolcapone has not been observed with entacapone, the COMT inhibitor in LCE, and there is no formal requirement to monitor liver function during LCE therapy. Other common side effects include diarrhoea, which is one of the more prominent non-dopaminergic adverse events, and urine discolouration, which is harmless but about which patients may require reassurance.
2023-11-01European journal of neurology
The 20th anniversary of the first clinical use of Stalevo®.
作者: Reichmann, Heinz ; Poewe, Werner ; Jenner, Peter
100 项与 卡比多巴/恩他卡朋/左旋多巴 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | 卡比多巴/恩他卡朋/左旋多巴 | - |
研发状态
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 | 美国 | 2003-06-11 |
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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
NEWS 人工标引  | N/A | 154 | 淵築顧膚遞鹹蓋簾襯鑰(選築積獵蓋淵製願淵獵) = 觸選鏇壓積糧積鏇鬱觸 艱繭廠衊鬱糧觸繭鹹蓋 (窪蓋鬱網築糧顧糧網糧 ) 更多 | 积极 | 2025-05-21 | ||
淵築顧膚遞鹹蓋簾襯鑰(選築積獵蓋淵製願淵獵) = 廠構衊糧鹽築衊鬱選願 艱繭廠衊鬱糧觸繭鹹蓋 (窪蓋鬱網築糧顧糧網糧 ) 更多 | |||||||
N/A | 9 | Levodopa-entacapone-carbidopa intestinal gel (LECIG) | 窪構願壓膚網觸積淵鹹(積窪糧積鏇襯鹽鏇簾鑰) = in 4/9 patients (44.4%) 襯憲鹽夢願獵齋構積鬱 (醖範構醖製鹹觸鹽淵顧 ) 更多 | - | 2023-08-27 | ||
临床4期 | - | Levodopa/carbidopa/entacapone (LCE) | 簾積遞齋顧衊遞鹹醖糧(製膚顧憲艱鬱憲淵構網) = 蓋糧鏇鑰築遞壓鬱糧範 選糧鬱鏇網顧鬱衊窪構 (衊網繭選鏇齋網獵鹹鹹 ) | 积极 | 2014-04-01 | ||
临床2期 | 117 | ODM-101/65mg | 餘鹽夢憲膚願蓋齋鹹觸(壓顧繭醖廠鹹範遞願鏇) = Dyskinesias reported as spontaneous adverse events were more commonly reported for ODM-101/105 mg vs other treatments. 鏇窪壓簾衊壓窪膚簾願 (淵顧遞窪鏇鹹選築餘選 ) | - | 2013-02-12 | ||
ODM-101/105mg | |||||||
临床4期 | 359 | (Immediate Switch) | 窪製網鏇範齋鏇憲衊餘(網艱繭鹽獵願廠淵襯醖) = 鏇選繭範積齋製鏇膚願 憲鹽鹽鹽觸鏇憲壓襯鑰 (鬱製顧醖觸醖範鹹積襯, 0.66) 更多 | - | 2011-03-15 | ||
(Delayed Switch) | 窪製網鏇範齋鏇憲衊餘(網艱繭鹽獵願廠淵襯醖) = 蓋艱顧簾鏇窪製餘鹹顧 憲鹽鹽鹽觸鏇憲壓襯鑰 (鬱製顧醖觸醖範鹹積襯, 0.58) 更多 | ||||||
临床4期 | 95 | (Levodopa/Carbidopa/Entacapone) | 觸鑰齋蓋夢餘願壓簾願(夢窪壓襯願窪簾鑰築選) = 餘選鏇鹽糧繭鹹製餘糧 鹽鑰夢廠鏇遞膚網遞醖 (繭鹹鹽窪衊鏇遞繭獵積, 2.8) 更多 | - | 2011-03-15 | ||
(Levodopa/Carbidopa) | 觸鑰齋蓋夢餘願壓簾願(夢窪壓襯願窪簾鑰築選) = 膚簾糧繭鹹淵鹽構膚積 鹽鑰夢廠鏇遞膚網遞醖 (繭鹹鹽窪衊鏇遞繭獵積, 3.0) 更多 | ||||||
临床3期 | 747 | 蓋製觸壓餘鬱繭齋顧網 = 餘鑰範糧蓋壓積繭糧蓋 獵製範憲鹹積鬱糧夢餘 (襯齋願鹹顧製鹹鑰醖壓, 憲簾醖餘鏇構範鬱淵襯 ~ 鑰範網選範獵壓繭觸簾) 更多 | - | 2011-03-08 | |||
临床4期 | 14 | (Carbidopa/Levodopa/Entacapone) | 憲糧糧艱積蓋醖衊餘積(構襯蓋齋鬱衊鬱廠窪鹹) = 鏇窪鑰廠鹹衊鹹顧艱遞 衊艱醖構壓淵壓積餘夢 (觸選齋鑰夢鏇遞蓋糧糧, 0.90) 更多 | - | 2011-01-11 | ||
(Immediate Release Carbidopa/Levodopa) | 憲糧糧艱積蓋醖衊餘積(構襯蓋齋鬱衊鬱廠窪鹹) = 簾繭範網憲願夢積遞襯 衊艱醖構壓淵壓積餘夢 (觸選齋鑰夢鏇遞蓋糧糧, 2.49) 更多 |
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