Drug intelligence / Profile preview

opelconazole

Development stage
Phase 3
Lead developer
Pulmocide
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Inhalation
01

Overview

Opelconazole is a synthetic triazole antifungal agent developed for inhaled administration, primarily targeting pulmonary fungal infections such as invasive pulmonary aspergillosis. It acts by selectively binding to and inhibiting the CYP450-dependent 14-alpha-sterol demethylase (also known as lanosterol 14α-demethylase) in fungi, thereby blocking ergosterol synthesis—an essential component of the fungal cell membrane. This disruption leads to fungal cell lysis and inhibits infection in the lungs. Opelconazole is designed for high lung retention with minimal systemic exposure, aiming to improve efficacy while reducing systemic side effects and drug-drug interactions commonly seen with other antifungals. The drug has shown potential utility in patients who have failed previous antifungal treatments and has received Orphan Drug, Fast Track, and Qualified Infectious Disease Product designations from regulatory agencies[1][2][3][7][8].

Other names
opelconazole(inn)opelconazole [USAN]1931946-73-4
02

Targets

CYP51A1 (Sterol 14α-demethylase)

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