Itraconazole

Itraconazole is a broad-spectrum triazole antifungal agent widely used in clinical and research applications for its ability to inhibit fungal ergosterol synthesis by targeting the cytochrome P450 enzyme lanosterol 14alpha-demethylase and compromising the cell membrane, which leads to its fungicidal activity. It is effective against a range of pathogenic fungi, including Aspergillus, Candida, and Histoplasma species, making it valuable for studying antifungal mechanisms and resistance. Beyond its antifungal properties, Itraconazole has anti-angiogenic and Hedgehog pathway-inhibiting effects and has gained interest in cancer research. Itraconazole has inhibitory activity on Smoothened (SMO) at different binding site to cyclopamine, thereby disrupting the signaling in Hedgehog pathway. It has been extensively investigated for its potential repurposing across various cancers, such as basal cell carcinoma, prostate cancer, non-small cell lung cancer, breast cancer, medulloblastoma, glioblastoma and pancreatic cancer.