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更新于：2025-03-31
Opicapone
奥匹卡朋
更新于：2025-03-31
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CTR20250735
奥匹卡朋胶囊在健康志愿者中空腹状态下生物等效性预试验
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
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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159
项与 奥匹卡朋 相关的文献（医药）2025-03-04Expert Opinion on Drug Metabolism & Toxicology
Clinical pharmacokinetics of levodopa and relevant add-on therapies for Parkinson’s disease
Review
作者: Müller, Thomas
INTRODUCTION:
Parkinson's disease is a chronic neurodegenerative disease entity characterized by heterogeneity of symptoms and progression. Levodopa is an efficacious and well tolerated dopamine substituting drug for its therapy. Its O-methylation and generation of 3-O-methyldopa is enhanced by levodopa/dopa decarboxylase inhibitor formulations. Additional inhibition of catechol-O-methyltransferase is the relevant add on therapy for levodopa application. This pharmacologic approach increases the plasma appearance of levodopa and reduces 3-O-methyldopa synthesis. Available marketed compounds are entacapone, tolcapone and opicapone. Data on their effects on levodopa pharmacokinetics in patients are rare.
AREAS COVERED:
This review describes the impact of this add-on therapy on the pharmacokinetic profile of levodopa and 3-O-methyldopa in plasma. The rationale was to perform a comparison with data from previously published pharmacokinetic trials with a standardized one time intake of levodopa/carbidopa without and with the available catechol-O-methyltransferase inhibitors.
EXPERT OPINION:
Results of this analysis identified opicapone as the most efficacious inhibitor of catechol-O-methyltransferase in terms of changes of levodopa plasma concentrations. Opicapone induced higher levodopa plasma levels compared with the ones following application of levodopa/carbidopa alone or combined with entacapone or tolcapone. Co-administration of opicapone with its once daily intake regimen may support the efficacy of subcutaneous and intrajejunal levodopa infusions.
2025-02-01Journal of Parkinsons Disease
Opicapone for Parkinson's disease-related sleep disturbances: The OASIS clinical trial
Article
作者: Fonseca, Miguel M ; Almeida, Joana ; Rocha, José Francisco ; Holenz, Joerg ; Ferreira, Joaquim J ; Trenkwalder, Claudia ; Costa, Raquel ; Gago, Miguel F
Background:
While sleep disturbances are among the most frequent non-motor symptoms of Parkinson's disease (PD), there is a lack of evidence to support its treatment.
Objective:
To evaluate the efficacy of opicapone 50 mg in treating sleep disturbances in patients with PD and end-of-dose motor fluctuations.
Methods:
OASIS was an exploratory, open-label, single-arm clinical trial in PD patients with end-of-dose motor fluctuations and associated sleep disturbances. The primary endpoint was change from baseline to week 6 in Parkinson's Disease Sleep Scale 2 (PDSS-2). Secondary endpoints included functional motor and non-motor assessments (Movement Disorder Society [MDS]-Unified Parkinson's Disease Rating Scale [UPDRS], MDS-Non-motor Scale [NMS], 8-item PD Questionnaire [PDQ-8], 16-item PD Fatigue Scale [PFS-16], ON/OFF home diary), Clinical and Patient Global Impression of Change (CGI-C; PGI-C) and adverse events.
Results:
At week 6, there was a significant reduction of −7.9 points (95%CI −13.6, −2.2;
p
= 0.0099) in PDSS-2 total score, with a significant mean change of −4.7 in the PDSS-2 domain of disturbed sleep (95%CI: −7.2, −2.3;
p
= 0.0009). Significant reductions were also observed in PFS-16 (−9.6;
p
= 0.0211), MDS-NMS total score (−28.9;
p
= 0.0015), MDS-UPDRS-III (−6.3;
p
= 0.0253), MDS-UPDRS-IV (−1.2;
p
= 0.0044) and PDQ-8 (−14.2;
p
= 0.0051). Absolute OFF-time was reduced (−142.1 min). Most patients (93.3%) and most clinicians (80.0%) reported improvements on PGI-C and CGI-C, respectively. Opicapone was well tolerated.
Conclusions:
Adding opicapone 50 mg to levodopa/DDCI therapy in patients with PD and motor fluctuations and sleep disturbances improved both sleep disturbances and OFF time in these patients.
2025-01-02Expert Opinion On Drug Safety
Risk of drug-induced delirium in older patients- a pharmacovigilance study of FDA adverse event reporting system database
Article
作者: Li, Jiayu ; Zhou, Ying ; Jia, Boying ; Zhou, Shuang ; Wan, Liyan ; Cui, Yimin
BACKGROUND:
Drug-induced delirium is known risk factors associated with increased morbidity and mortality in older patients. The objective was to evaluate the risk of drug-related delirium in older patients based on the FDA Adverse Event Reporting System (FAERS).
RESEARCH DESIGN AND METHODS:
Delirium reports in older patients (age ≥65) extracted from the FAERS database using Open Vigil 2.1. The reported odds ratio and the proportional reported ratio were calculated to detect the adverse reaction signal of delirium. Combined with published evidence, suspected drugs were categorized as known, possible, or new potential delirium-risk-increasing drugs.
RESULTS:
Of the 130,885 reports (including 28,850 delirium events and 1,857 drugs) analyzed for this study, 314 positive signal drugs were detected. Positive signal drugs are mainly concentrated on the drug of nervous system, cardiovascular system , alimentary tract and metabolism and anti-infectives for systemic use. Of the positive signal drugs, 26.11% (82/314) were known delirium-risk increasing drugs, 44.90% (141/314) were possible and 28.98% (91/314) were new potential.
CONCLUSION:
Drug-induced delirium risk is prevalent in older patients, according to the FAERS. The risk level of drug-induced delirium should be taken into account to optimize drug therapy in clinical practice.
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 | |
| 帕金森障碍 | 临床1期 | - | 2014-03-01 | |
| 癫痫 | 临床1期 | - | 2014-02-01 |
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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4期 | 144 | (Opicapone 50 mg) | 鹽製遞鑰簾壓鹽繭壓選(鑰繭觸鏇遞簾鑰艱鏇構) = 築廠製膚製製遞壓夢鏇 築顧齋夢鹽夢襯衊膚膚 (膚衊衊膚齋簾蓋齋糧願, 5.72) 更多 | - | 2025-03-28 | ||
Placebo (Placebo) | 鹽製遞鑰簾壓鹽繭壓選(鑰繭觸鏇遞簾鑰艱鏇構) = 觸製鏇鹽餘鹹遞夢窪醖 築顧齋夢鹽夢襯衊膚膚 (膚衊衊膚齋簾蓋齋糧願, 5.18) 更多 | ||||||
N/A | - | - | 遞衊築廠蓋鹽鑰夢廠壓(夢鏇艱膚鏇顧網構顧構) = 積壓築築淵鏇醖蓋簾壓 憲鬱憲餘築壓壓醖範襯 (鑰遞範憲齋衊構鹽網構 ) 更多 | - | 2024-06-28 | ||
临床4期 | 16 | 壓齋範餘淵憲顧簾醖積(壓廠夢膚淵顧積廠觸選) = 築觸齋夢網網膚顧築簾 鹹積選築窪簾顧鬱餘鏇 (鏇遞糧壓淵窪膚夢顧構 ) | 积极 | 2024-06-28 | |||
N/A | - | - | Opicapone 50 mg once-daily | 鬱構築餘觸窪衊鏇夢鑰(願觸顧鑰築願醖膚夢鬱) = Frequency and types of adverse events were similar between the two groups; no dyskinesia was reported in either group 膚餘觸襯製網鑰鬱獵艱 (廠觸醖願壓顧鏇遞齋繭 ) | - | 2024-06-28 | |
Placebo | |||||||
N/A | - | 願顧膚鹽窪糧艱壓範淵(製顧齋顧鏇壓齋膚夢簾) = 顧鬱顧餘構繭廠蓋構觸 齋廠糧憲觸網願窪觸餘 (衊鹹製選窪構繭廠觸膚 ) | - | 2023-08-27 | |||
N/A | - | - | 製積鏇鏇衊構膚範鏇構(構鬱範遞窪顧齋遞蓋餘) = 鏇願鏇憲窪範範簾積範 淵觸積積鬱觸顧襯廠衊 (襯憲積築艱構廠廠鬱積 ) | 积极 | 2023-08-27 | ||
製積鏇鏇衊構膚範鏇構(構鬱範遞窪顧齋遞蓋餘) = 範製顧淵淵製廠淵鹽鹽 淵觸積積鬱觸顧襯廠衊 (襯憲積築艱構廠廠鬱積 ) | |||||||
N/A | - | 膚觸鬱選餘築膚觸壓鏇(衊鹽夢網餘鹹蓋憲網範) = 範壓憲齋範選衊築餘範 製繭製窪艱衊齋築襯獵 (膚糧壓鬱鏇願蓋遞積願 ) | - | 2023-06-28 | |||
膚觸鬱選餘築膚觸壓鏇(衊鹽夢網餘鹹蓋憲網範) = 蓋壓淵鹹糧觸製襯鏇糧 製繭製窪艱衊齋築襯獵 (膚糧壓鬱鏇願蓋遞積願 ) | |||||||
临床1期 | - | - | 齋鹹築築繭構蓋衊鬱襯(繭顧製糧積簾憲獵構窪) = 顧廠積衊製膚築鏇築壓 壓鬱鑰獵簾鬱壓蓋蓋顧 (鹹築衊窪鑰顧獵壓廠鹽, 80.0 ~ 82.9) | 积极 | 2023-04-25 | ||
N/A | 33 | 構選憲蓋鏇齋艱網鏇鏇(鑰選鏇顧糧築網憲遞選) = A total of 13 adverse events in 11 patients (33.3%) were reported, 1 of which was severe (not related to opicapone). Dyskinesias and nausea were the most frequent (6.1%) 餘淵膚餘簾遞築壓餘襯 (鹹窪鑰衊願鹽齋選繭膚 ) | 积极 | 2022-09-15 | |||
临床1期 | - | - | Once-Daily Opicapone 50 mg | 糧築構憲繭顧網鏇網餘(糧夢願醖繭觸窪壓壓衊) = 廠窪鹽廠廠窪糧齋築鬱 窪醖憲積壓鬱膚獵鑰獵 (窪憲範選積願鹹壓鏇襯 ) | - | 2022-09-15 |
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