Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC 50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase ( cytochrome P450 enzyme ), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein ( OSBP ) inhibitor.
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