Drug intelligence / Profile preview

balovaptan + itraconazole

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

**balovaptan + itraconazole** is a combination of balovaptan, a selective small molecule antagonist of the vasopressin 1a receptor (V1aR), and itraconazole, a triazole antifungal agent and potent CYP3A4 inhibitor. Balovaptan is an investigational drug developed primarily for the treatment of autism spectrum disorder (ASD) due to its ability to modulate social behavior by reducing vasopressin signaling in the brain. Itraconazole, normally used for fungal infections, is employed in this context to inhibit CYP3A4, a major enzyme responsible for the metabolism of balovaptan, thereby increasing its systemic exposure. The combination has been studied in healthy volunteers to assess the pharmacokinetic interactions, showing that itraconazole increases balovaptan blood levels by at least 3.1-fold. Balovaptan is under development and has not yet been approved for clinical use, while itraconazole is an approved antifungal agent[1][2][4].

Other names
balovaptan + itraconazoleRO5285119 + itraconazole
02

Targets

CYP51A1 (Sterol 14α-demethylase)AVPR1A (Arginine vasopressin receptor 1A)CYP3A4 (Cytochrome P450 3A4)

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