Drug intelligence / Profile preview

seltorexant + itraconazole

Development stage
Unknown
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

**Seltorexant + itraconazole** is a combination of seltorexant, a small-molecule selective orexin receptor type-2 antagonist under development primarily for the treatment of major depressive disorder and insomnia, and itraconazole, an established antifungal agent that is a potent inhibitor of the CYP3A4 enzyme. Seltorexant blocks the orexin OX2 receptor, reducing arousal and promoting sleep, and is being investigated for both antidepressant and sleep-promoting effects[1][3][5][7]. Itraconazole, while an antifungal, is sometimes used in pharmacokinetic studies to characterize the drug interaction potential via inhibition of CYP3A4, which is the main metabolic pathway for seltorexant[3]. The combination may be studied in a pharmacokinetic context to assess the impact of CYP3A4 inhibition on seltorexant’s metabolism, exposure, and safety profile, not as a routine therapeutic combination.

02

Targets

HCRTR1 (Orexin/hypocretin receptor type 1)HCRTR2 (Orexin/hypocretin receptor type 2)CYP51A1 (Sterol 14α-demethylase)CYP3A4 (Cytochrome P450 3A4)

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