Hydroxy Itraconazole

Itraconazole metabolite Hydroxy Itraconazole is an active metabolite of Itraconazole (ITZ), which is a triazole antifungal agent.

Signaling Pathways >> Anti-infection >> Fungal

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Antifungal[1]

Hydroxy Itraconazole (OH-ITZ) is an active metabolite of Itraconazole (ITZ). Although OH-ITZ is also reported to have antifungal activity in vitro, its pharmacokinetics in humans has been studied less than that of ITZ. ITZ and OH-ITZ have a triazole ring and inhibit CYP3A. Their half-lives can be extended by 26-60% with repeated administration compared to single administration[1].

The plasma concentration of OH-ITZ is weakly dependent on the dose of ITZ, most likely because the process that forms OH-ITZ is saturated. Serum albumin and GFR may alter the pharmacokinetics of ITZ and OH-ITZ. Antifungal activity should be discussed while taking into account not only the plasma concentration of ITZ but also that of OH-ITZ. However, the pharmacokinetics of OH-ITZ is similar to that of ITZ in immunocompromised patients taking an oral solution of ITZ. Since the plasma concentrations of ITZ and OH-ITZ are closely correlated, determining the plasma concentration of either should be sufficient from a clinical point of view[1].

[1]. Mino Y, et al. Hydroxy-itraconazole pharmacokinetics is similar to that of itraconazole in immunocompromised patients receiving oral solution of itraconazole. Clin Chim Acta. 2013 Jan 16;415:128-32.

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