Itraconazole as a repurposed anti-cancer agent: focusing on synthesis, mechanisms of action and therapeutic insights

Abstract

Cancer drug development faces significant challenges due to long timelines, stringent regulatory requirements, and high failure rates. Drug repurposing has emerged as an efficient strategy to accelerate the discovery of novel therapies. Itraconazole (ITZ), a triazole antifungal approved in 1992 and widely used for over 30 years, has recently shown promising anticancer activity. This review provides a comprehensive overview of ITZ in cancer therapy, covering its synthesis and chemistry-based perspectives, mechanisms of action including angiogenesis inhibition and modulation of key signaling pathways, and preclinical and clinical evidence of its efficacy against various cancers. In addition, we discuss comparative drug delivery systems to optimize its therapeutic potential and summarize the latest studies from 2021 to 2025 highlighting its role as a potential anticancer agent. By consolidating current knowledge, this review aims to guide researchers and clinicians in exploring ITZ as a repurposed therapeutic option for cancer treatment.