Abstract: Itraconazole has potent anticancer activity at the standard therapeutic doses, which is proved in vitro and in vivo preclinical studies, even in active clinical trials. The precise mode of action of itraconazole for its anticancer activity has not been elucidated, however multiple putative mechanisms are proposed, such as antiangiogenesis, inhibition of Hedgehog pathway, autophagy induction and reversal of multidrug resistance. Its high efficacy, known toxicity and wellestablished pharmacokinetics make this generic drug a strong candidate for repurposing as an oncological treatment.

Key words: Itraconazole； Angiogenesis inhibitors； Signal transduction, Drug resistance, multiple