Drug intelligence / Profile preview

Hydroxy Itraconazole

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Hydroxy Itraconazole is an active metabolite of the antifungal drug itraconazole. It is formed in the body through the metabolism of itraconazole, primarily by the cytochrome P450 isoform 3A4 (CYP3A4) enzyme. Hydroxy Itraconazole exhibits in vitro antifungal activity comparable to its parent compound, itraconazole. It circulates in plasma at concentrations equal to or higher than itraconazole and contributes significantly to the overall antifungal efficacy. Its mechanism of action is believed to be similar to itraconazole, involving the inhibition of fungal lanosterol 14α-demethylase, which disrupts ergosterol synthesis in the fungal cell membrane. Beyond its antifungal properties, Hydroxy Itraconazole is also known to inhibit CYP3A, contributing to potential drug-drug interactions. It is a subject of research, including studies related to malignant tumors, and its plasma levels are often monitored in clinical settings to assess the effectiveness of itraconazole therapy.

Other names
Itraconazole metabolite Hydroxy Itraconazole
02

Targets

CYP3A4 (Cytochrome P450 3A4)CYP51A1 (Sterol 14α-demethylase)

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