Pitolisant-wakix efficacy and effects

Pitolisant (Pitolisant)-wakix is a first-class drug that acts on histamine H3 receptors (H3Rs) and is an antagonist/inverse agonist, which enhances the activation of histaminergic neurons and other neurotransmitters (i.e., dopamine, acetylcholine, norepinephrine) in the brain. Preclinical studies have shown that in narcolepsy orexin knockout mice, tilolixen tablets enhanced histamine and norepinephrine neuronal activity, increased arousal, and increased abnormal rapid eye movement (REM) sleep latency.

Narcolepsy is a rare sleep disorder characterized by excessive daytime sleepiness (EDS) and abnormal REM sleep manifestations (i.e., paroxysmal seizures, sleep paralysis, hypnagogic and hypnagogic hallucinations). Experimental data obtained in wild-type and orexin knockout mice and cats indicate that tilorisen tablets enhance arousal and reduce slow-wave sleep and sleep, thus confirming the possibility of using it to treat narcolepsy in humans. Because this mechanism of action is different from current treatments, tilolixen tablets may be an alternative medication for patients with narcolepsy. Effectiveness of tilolixen tablets compared with placebo in the treatment of major clinically relevant narcolepsy symptoms including cataplexy. Furthermore, tilolixen tablets demonstrated a safety profile compared with placebo and active controls, with headache, insomnia, and nausea being the major side effects.

Tilorisen tablets have been marketed in the country, but have not yet been included in medical insurance. The price of each box of the original version of tilorisen tablets marketed overseas may be over more than RMB 4,000 (the price may fluctuate due to exchange rates). Currently, there are no generic versions of tilorisen tablets produced and marketed overseas.