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Pitolisant: A Review in Narcolepsy with or without Cataplexy.
CNS Drugs ( IF 6 ) Pub Date : 2020-02-01 , DOI: 10.1007/s40263-020-00703-x
Yvette N Lamb 1
Affiliation  

Pitolisant (Wakix®), an orally available, first-in-class antagonist/inverse agonist of the histamine 3 receptor, is approved in the EU (as of March 2016) for the treatment of narcolepsy with or without cataplexy in adults and in the USA (as of August 2019) for the treatment of excessive daytime sleepiness (EDS) in adults with narcolepsy. Pitolisant was demonstrated to have minimal risk of abuse in preclinical and clinical studies, and is the only anti-narcoleptic drug not scheduled as a controlled substance in the USA. The totality of evidence from pivotal and supportive phase III trials suggests that pitolisant administered at up to the recommended maximum dose of 36 mg once daily reduces EDS and cataplexy in adults with narcolepsy relative to placebo. Noninferiority of pitolisant to modafinil in the management of EDS was not demonstrated. Pitolisant was generally well tolerated in clinical trials. Consistent with its mechanism of action, the most common treatment-emergent adverse events included headache, insomnia and anxiety. With minimal abuse potential and offering the convenience of oral, once-daily administration, pitolisant extends the range of approved treatment options available to adult patients with narcolepsy with or without cataplexy.

中文翻译:

Pitolisant:发作性睡病的回顾与否。

Pitolisant(Wakix®)是一种可口服的,组胺3受体的一流拮抗剂/反向激动剂,已获欧盟批准(截至2016年3月),用于成人和成人中发作性睡病的伴或不伴瘫痪的发作。美国(截至2019年8月)用于治疗发作性睡病成人过度白天嗜睡(EDS)。在临床前和临床研究中证明Pitolisant具有最低的滥用风险,并且是美国唯一未列为管制药物的抗麻醉药。来自关键性和支持性III期临床试验的全部证据表明,与推荐的安慰剂相比,发作性睡病的成年人每天服用最高建议最大剂量36 mg的pitolisant可以降低EDS和昏厥。在EDS的治疗中未证实匹立莫司对莫达非尼的不劣效性。临床试验中普遍耐受性好。与它的作用机制一致,最常见的治疗性不良事件包括头痛,失眠和焦虑。pitolisant具有最小的滥用可能性,并且为口服,每天一次的给药提供了便利,从而扩大了已批准的发作性睡病伴或不伴有猝倒症的成年患者的治疗选择范围。
更新日期:2020-01-29
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