Drug intelligence / Profile preview

nivasorexant

Development stage
Phase 2
Lead developer
Idorsia
Modality
Small Molecules
Administration
Oral
01

Overview

Nivasorexant (developmental code name ACT-539313) is an orally active small-molecule drug that acts as a selective antagonist of the orexin 1 receptor (OX1R). It was developed for central nervous system disorders such as binge eating disorder and anxiety disorders. Nivasorexant is brain-penetrating and exhibits high selectivity for OX1R over OX2R (approximately 60-fold lower potency at OX2R), with a mean elimination half-life of about 3.3–6.5 hours. The mechanism of action involves antagonism of the orexin 1 receptor, which is implicated in regulating arousal and reward-related behaviors; selective antagonism may provide efficacy in behavioral disorders without promoting sleepiness typical of dual orexin antagonists. The drug was originally discovered by Actelion Pharmaceuticals and further developed by Idorsia Pharmaceuticals[1][2][4][5].

Other names
nivasorexantACT-539313ACT539313ACT 539313SORA
02

Targets

CYP3A4 (Cytochrome P450 3A4)HCRTR1 (Orexin/hypocretin receptor type 1)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)CYP2C19 (Cytochrome P450 2C19)

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