seltorexant

Seltorexant is a selective antagonist of the human orexin-2 receptor (OX2R). Orexin is a neuropeptide that regulates wakefulness, and inhibiting orexin receptor signaling promotes sleep. Seltorexant is being developed as an adjunctive treatment for major depressive disorder (MDD) with insomnia symptoms, where it has demonstrated statistically significant and clinically meaningful improvements in both depressive symptoms and sleep disturbance outcomes in phase 3 trials. It is also under investigation for other indications such as insomnia and agitation/aggression in Alzheimer's disease. Seltorexant was originally discovered by Minerva Neurosciences and further developed by Janssen, which now leads its development[1][2][5][6]. Seltorexant distinguishes itself from other approved orexin antagonists by selectively blocking only the OX2 receptor, rather than both OX1 and OX2 receptors like dual orexin receptor antagonists (DORAs) such as suvorexant or lemborexant[5][6]. Its pharmacokinetics are considered ideal for sleep induction due to rapid absorption and short half-life.

Other names

seltorexant