Drug intelligence / Profile preview

itraconazole

Development stage
Approved
Lead developer
OMJ Pharmaceuticals
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Itraconazole is a broad-spectrum triazole antifungal agent used to treat a variety of fungal infections including aspergillosis, blastomycosis (Gilchrist’s disease), coccidioidomycosis (valley fever), histoplasmosis (Darling’s disease), paracoccidioidomycosis, sporotrichosis, and onychomycosis. It is also used for oropharyngeal and esophageal candidiasis. Itraconazole works by inhibiting the fungal cytochrome P-450-dependent enzyme lanosterol 14α-demethylase (ergosterol synthesis enzyme), leading to impaired ergosterol synthesis in the fungal cell membrane and thus inhibiting fungal growth. It can be administered orally as capsules or solution and intravenously. Itraconazole has been explored for off-label uses such as certain cancers due to its inhibition of the hedgehog signaling pathway[1][2][3][6][9].

Brand names
SporanoxTolsuraOnmel斯皮仁诺适扑诺
Other names
伊曲康唑
02

Targets

CYP51A1 (Sterol 14α-demethylase)

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