关键词: 替洛利生, 发作性睡病, H3受体反向激动剂

Abstract: Pitolisant, a selective histamine H? receptor inverse agonist, promotes wakefulness by blocking H? autoreceptor-mediated feedback inhibition to elevate central histamine levels. It is clinically indicated for wake promotion in narcolepsy. The development journey of pitolisant spans over two decades, encompassing extensive preclinical and clinical research. These studies have demonstrated both sustained efficacy in managing narcolepsy and a favorable long-term safety profile.Notably, pitolisant received formal marketing authorization from China's National Medical Products Administration (NMPA) for treating excessive daytime sleepiness or cataplexy in adult narcolepsy patients. This approval addresses an unmet medical need in China's therapeutic landscape, providing patients with a safe, effective, and well-tolerated novel therapeutic option.

Key words: Pitolisant, Narcolepsy, H3 receptor inverse agonist