Drug intelligence / Profile preview

orvepitant + itraconazole

Development stage
Unknown
Lead developer
NeRRe Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Orvepitant + itraconazole is a hypothetical or investigational drug combination composed of orvepitant, a neurokinin-1 (NK1) receptor antagonist, and itraconazole, an azole antifungal agent. **Orvepitant** acts primarily as an NK1 receptor antagonist and has been developed mainly for the treatment of conditions such as major depressive disorder and chemotherapy-induced nausea and vomiting by modulating substance P activity. **Itraconazole** is a well-established azole class antifungal that inhibits fungal ergosterol synthesis by blocking the enzyme 14α-demethylase, resulting in increased cellular membrane permeability and fungal death. No clinical trials, product information, or standard indication currently exist for the combination of orvepitant and itraconazole. Notably, the combination could raise significant drug-drug interaction concerns because itraconazole is a strong inhibitor of CYP3A4, potentially increasing exposure to orvepitant, which is metabolized by this pathway. There is no established indication or clinical precedent for this particular combination.

02

Targets

TACR1 (Neurokinin‑1 Receptor)CYP3A4 (Cytochrome P450 3A4)CYP51A1 (Sterol 14α-demethylase)

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