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IPX066:一种新型卡比多巴-左旋多巴控释制剂。

IPX066: a novel carbidopa-levodopa extended-release formulation.

机构信息

University of South Florida Parkinson's Disease and Movement Disorders Center, NPF Center of Excellence, Byrd Institute, 4001 E. Fletcher Ave, 6th Floor, Tampa, FL 33613, USA.

出版信息

Expert Rev Neurother. 2012 Feb;12(2):133-40. doi: 10.1586/ern.11.195.

Abstract

Levodopa (LD) remains the most effective medication to treat Parkinson's disease (PD). However, most patients develop motor fluctuations and dyskinesias with long-term LD use. It is thought that these response complications are due, at least in part, to LD's short half-life. Thus, there is great interest in long-acting LD preparations that might be able to provide robust antiparkinsonian benefit through the day and potentially avoid the development of motor fluctuations and dyskinesias. IPX066 is an investigational extended-release carbidopa-levodopa (CD-LD) formulation. It is designed to achieve rapid absorption and onset of clinical benefit, similar to CD-LD immediate release, and to provide more sustained therapeutic LD levels and longer duration of clinical benefit. In Phase III clinical trials, IPX066 was demonstrated to be efficacious in early PD compared with placebo, and in moderate-to-advanced PD, it provided more sustained clinical benefit with fewer dose administrations than CD-LD immediate release, as reported in published abstracts.

摘要

左旋多巴(LD)仍然是治疗帕金森病(PD)最有效的药物。然而,大多数患者在长期使用 LD 后会出现运动波动和运动障碍。人们认为,这些反应并发症至少部分是由于 LD 的半衰期短。因此,人们对长效 LD 制剂非常感兴趣,这些制剂可能能够在一天中提供强大的抗帕金森病益处,并有可能避免运动波动和运动障碍的发展。IPX066 是一种研究性的控释卡比多巴-左旋多巴(CD-LD)制剂。它旨在实现快速吸收和临床获益的快速起效,类似于 CD-LD 速释制剂,并提供更持久的治疗性 LD 水平和更长的临床获益持续时间。在 III 期临床试验中,与安慰剂相比,IPX066 被证明在早期 PD 中有效,在中重度至晚期 PD 中,与 CD-LD 速释制剂相比,它提供了更持久的临床获益,并且给药次数更少,这在已发表的摘要中有所报道。

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