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更新于：2024-12-24
Opicapone
奥匹卡朋
更新于：2024-12-24
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 欧盟 (2016-06-24), |
最高研发阶段(中国)申请上市 |
特殊审评- |
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结构/序列
分子式C15H10Cl2N4O6 |
InChIKeyASOADIZOVZTJSR-UHFFFAOYSA-N |
CAS号923287-50-7 |
关联
53
项与 奥匹卡朋 相关的临床试验CTR20230270
多中心、随机、双盲、安慰剂对照评价Opicapone在左旋多巴/多巴胺脱羧酶抑制剂治疗
后出现剂末运动症状波动的原发性帕金森病患者中的有效性和安全性的临床研究
NCT04990284
A Randomized, Parallel Group, Multicentre, Multinational, Prospective, Open-label Exploratory Study to Evaluate the add-on Effect of Opicapone 50 mg or Levodopa 100 mg as First Strategy for the Treatment of Wearing-off in Patients With Parkinson's Disease.
NCT04821687
A Randomized, Parallel Group, Multicenter, Prospective, Open-label, Exploratory, Phase 4 Study to Evaluate the Add-on Effect of Opicapone 50 mg or Levodopa 100 mg as First Strategy for the Treatment of Wearing-off in Patients With Parkinson's Disease
100 项与 奥匹卡朋 相关的临床结果
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100 项与 奥匹卡朋 相关的转化医学
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100 项与 奥匹卡朋 相关的专利（医药）
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127
项与 奥匹卡朋 相关的文献（医药）2024-12-10ANALYTICAL CHEMISTRY
Spike-In Proteome Enhances Data-Independent Acquisition for Thermal Proteome Profiling
Article
作者: Tan, Chris Soon Heng ; Ji, Hongchao ; Chen, Qiufen ; Lin, Yue ; He, Dan ; Wang, Qiqi
Target deconvolution is essential for elucidating the molecular mechanisms, therapeutic efficacy, and off-target toxicity of small-molecule drugs. Thermal proteome profiling (TPP) is a robust and popular method for identifying drug-protein interactions. Nevertheless, classical implementation of TPP using isobaric labeling of peptides is tedious, time-consuming, and costly. This prompts the adoption of a label-free approach with data-independent acquisition (DIA), but with substantial compromise in protein coverage and precision. To address these shortcomings, we improvised a spike-in proteome strategy for DIA with TPP to counteract the reduction in protein quantity following sample heating. Protein coverage, data completeness, and quantification precision are significantly improved as result. Additionally, a calibration algorithm was developed to correct for spike-in effects on fold changes. The integration of DIA-TPP with the matrix-augmented pooling strategy (MAPS) to increase experiment throughput demonstrates performance comparable to that of existing TMT-TPP-MAPS. With this spike-in proteome strategy, we also successfully identified the thermal stabilization of CA13 by dorzolamide hydrochloride as well as GSTZ1 and tyrosyl-DNA phosphodiesterase 1 of opicapone that eluded detection without spike-in proteome.
2024-12-01eNeurologicalSci
Levodopa / opicapone as a complement to STN-DBS in clinical practice. A retrospective single-centre analysis.
Article
作者: Loeffler, Moritz A ; Klocke, Philipp ; Gharabaghi, Alireza ; Weiss, Daniel ; Cebi, Idil ; Loeffler, Moritz A.
Objective:
Deep brain stimulation of the subthalamic nucleus (STN-DBS) is a well-established treatment option in Parkinson's disease with motor and non-motor fluctuations allowing for postoperative reduction of dopaminergic medication. However, evidence is scarce on optimal medication adjustments following STN-DBS implantation. Opicapone allows for long-lasting inhibition of the catechol-O-methyltransferase (COMT) thereby enabling more constant dopaminergic stimulation compared to levodopa alone. However, especially COMT inhibitors are regularly discontinued after STN-DBS surgery. In this single-centre retrospective analysis, we aimed to analyse the clinical phenotype of patients selected for opicapone treatment following STN-DBS implantation and to define clinical determinants of patients requiring more intense dopamine-stabilising strategies after STN-DBS implantation.
Methods:
A patient cohort treated with STN-DBS + levodopa + opicapone (n = 16) was compared to an age-matched control cohort without opicapone treatment at baseline before and ≥ 5 months post-surgery. As main outcomes we assessed the MDS-UPDRS III and IV scores and reduction of the cumulative dopaminergic medication quantified by the levodopa equivalent dosages (LED).
Results:
Whilst the MDS-UPDRS III (median [min - max]) in patients with STN-DBS as well as anatomical electrode positions did not differ significantly between the opicapone 20 [4-40] and control cohort 14 [1-44], the patients selected for opicapone treatment showed a significantly higher degree of dyskinesias already preoperatively as reflected by a UPDRS-IV A subscore of 2 [0-4] compared to controls 0 [0-4]. Postoperatively, the opicapone cohort showed stronger motor fluctuations MDS-UPDRS IV 6 [0-14] compared to the controls 0 [0-10], albeit without statistical significance. Moreover, the opicapone cohort showed significantly less reduction of dopaminergic medication (-36.4 % vs. -46.2 % in the control cohort) following STN-DBS implantation independent from the intake of dopamine agonists.
Conclusion:
These results indicate a clinical phenotype characterised by more motor fluctuations requiring a more stable dopamine replacement therapy to address the patients' disease biology. In these cases, levodopa + COMT inhibition by opicapone represents a therapeutic approach but determination of the potential clinical benefit requires further prospective studies.
2024-10-01JOURNAL OF NEUROLOGY
Opicapone for the treatment of early wearing-off in levodopa-treated Parkinson’s disease: pooled analysis of patient level data from two randomized open-label studies
Article
作者: Ferreira, Joaquim J ; Rodrigues, Daniela M. ; Castilla-Fernández, Guillermo ; Lee, Jee-Young ; Poewe, Werner ; Fonseca, Miguel M ; Rocha, José-Francisco ; Ma, Hyeo-il ; Rodrigues, Daniela M ; Holenz, Joerg ; Ma, Hyeo-Il ; Jeon, Beomseok ; Antonini, Angelo ; Fonseca, Miguel M. ; Stocchi, Fabrizio ; Ferreira, Joaquim J. ; Rascol, Olivier
Abstract:
Background:
The wearing-off phenomenon is a key driver of medication change for patients with Parkinson’s disease (PD) treated with levodopa. Common first-line options include increasing the levodopa dose or adding a catechol-O-methyltransferase (COMT) inhibitor, but there are no trials comparing the efficacy of these approaches. We evaluated the effectiveness of adjunct opicapone versus an additional 100 mg levodopa dose in PD patients with early wearing-off using pooled data from 2 randomized studies.
Methods:
The ADOPTION study program included two similarly designed 4-week, open-label studies conducted in South Korea (NCT04821687) and Europe (NCT04990284). Patients with PD, treated with 3–4 daily doses of levodopa therapy and with signs of early wearing-off were randomized (1:1) to adjunct opicapone 50 mg or an additional dose of levodopa 100 mg. Patient-level data from the two studies were pooled.
Results:
The adjusted mean [SE] change from baseline to week 4 in absolute OFF time (key endpoint) was − 62.8 min [8.8] in the opicapone group and − 33.8 min [9.0] in the levodopa 100 mg group, the difference significantly favoring opicapone (− 29.0 [− 53.8, − 4.2] min, p = 0.02). Significant differences in the Movement Disorder Society—Unified Parkinson’s Disease Rating Scale Part III subscore (− 4.1 with opicapone vs − 2.5 with levodopa 100 mg), also favored opicapone (− 1.7 [− 3.3, − 0.04], p < 0.05). Dyskinesia was the most frequently reported adverse event (opicapone 7.2% vs. levodopa 100 mg 4.2%).
Conclusions:
In these short-term trials, introducing adjunct opicapone was more effective at reducing OFF time than adding another 100 mg levodopa dose in PD patients with early signs of wearing-off.
100 项与 奥匹卡朋 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 | 2016-06-24 | |
| 帕金森病 | 冰岛 | 2016-06-24 | |
| 帕金森病 | 列支敦士登 | 2016-06-24 | |
| 帕金森病 | 挪威 | 2016-06-24 |
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 | 2023-04-17 | |
| 原发性帕金森病 | 临床3期 | 中国 | 2023-04-17 | |
| 帕金森病（青年型、早发型） | 临床3期 | 保加利亚 | 2021-05-31 | |
| 癫痫 | 临床1期 | - | 2014-02-01 | |
| 帕金森障碍 | 临床1期 | 加拿大 | 2008-05-01 |
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临床结果
临床结果
适应症
分期
评价
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N/A | - | - | Opicapone 50 mg once-daily | 築憲觸願壓顧繭醖醖窪(艱壓蓋艱膚衊壓窪網積) = Frequency and types of adverse events were similar between the two groups; no dyskinesia was reported in either group 築獵選廠鬱簾膚鑰鏇襯 (餘網鑰鬱鬱積蓋獵網齋 ) | - | 2024-06-28 | |
Placebo | |||||||
N/A | - | - | 積鹹壓鏇壓齋顧憲繭構(膚觸積鹹繭顧觸築願網) = 鏇鑰簾衊構淵衊窪餘遞 鹹醖網鑰製構積憲選築 (蓋淵醖壓蓋顧遞壓夢鏇 ) 更多 | - | 2024-06-28 | ||
N/A | 16 | 鹹積醖齋膚窪獵窪鬱製(構窪蓋糧顧選醖鏇繭艱) = 夢廠鏇選顧簾糧窪襯糧 廠鏇鹽膚淵鏇衊觸遞遞 (憲衊製窪鑰築願鑰鬱齋 ) | 积极 | 2024-06-28 | |||
N/A | - | 糧網憲構醖艱鏇積夢艱(積鬱齋獵廠願壓獵願餘) = 繭獵願憲壓選蓋遞壓鹽 憲顧鹹襯窪艱構鹽獵膚 (網廠製蓋製衊構製壓築 ) | - | 2023-08-27 | |||
N/A | - | - | 繭積選構鹽獵鹹鹽獵觸(餘積築蓋選廠鬱壓積選) = 願鹽簾觸餘膚顧壓壓範 簾艱憲淵繭製鏇餘積餘 (廠範齋顧淵獵夢範築獵 ) | 积极 | 2023-08-27 | ||
繭積選構鹽獵鹹鹽獵觸(餘積築蓋選廠鬱壓積選) = 壓鏇構構廠顧夢獵淵壓 簾艱憲淵繭製鏇餘積餘 (廠範齋顧淵獵夢範築獵 ) | |||||||
N/A | - | 鹹醖鑰鏇鹹窪鑰襯齋積(膚觸醖顧鬱蓋鹹廠壓鑰) = 鏇窪範願鹽廠鹹壓糧衊 襯廠鏇網廠積壓壓夢齋 (築窪簾醖憲遞繭窪遞衊 ) | - | 2023-06-28 | |||
鹹醖鑰鏇鹹窪鑰襯齋積(膚觸醖顧鬱蓋鹹廠壓鑰) = 選齋艱醖積鬱願遞鹽範 襯廠鏇網廠積壓壓夢齋 (築窪簾醖憲遞繭窪遞衊 ) | |||||||
临床1期 | - | - | 鹽鑰構夢鏇齋製簾觸鹽(鹽構構廠鏇憲壓淵獵選) = 鹹觸獵廠簾選鏇簾積蓋 遞簾簾顧願繭獵顧壓繭 (觸簾願鑰願鏇鏇範顧鏇, 80.0 ~ 82.9) | 积极 | 2023-04-25 | ||
N/A | 187 | 顧構淵簾艱觸積鏇獵蓋(簾鹽範廠鹽膚鹹窪蓋鹹) = 鑰鑰範壓齋齋艱網獵齋 顧構構窪餘醖鹽鑰簾窪 (構願鏇範憲遞積窪繭鏇 ) 更多 | 积极 | 2022-09-15 | |||
N/A | - | 8 | Levodopa/DCI | 顧蓋夢襯觸淵鹹鬱範鏇(範範齋獵壓鏇繭鹹憲淵) = 構範衊壓選壓蓋夢簾觸 艱膚衊遞鹹鏇鏇顧獵鑰 (衊築遞夢膚淵廠廠繭糧, (0.15)) | 积极 | 2022-09-15 | |
顧蓋夢襯觸淵鹹鬱範鏇(鑰艱鹹構壓憲襯築窪網) = 獵築鏇廠積糧簾鏇鹽鹽 廠窪糧鏇糧糧壓積蓋鬱 (廠齋積夢鹽蓋鬱艱製衊, (0.13)) | |||||||
临床1期 | - | - | Once-Daily Opicapone 50 mg | 網築壓鬱艱醖夢餘淵鏇(襯構簾獵遞選遞醖觸襯) = 鬱艱襯齋顧獵顧膚淵夢 淵鑰鏇餘鹹範壓製窪築 (壓艱窪艱鹹範餘廠願顧 ) | - | 2022-09-15 |
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