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Cisplatin + gemcitabine + itraconazole is an investigational combination chemotherapy regimen evaluated for the treatment of metastatic squamous non-small cell lung cancer (NSCLC). This regimen combines two standard cytotoxic agents—cisplatin, a platinum-based DNA crosslinking agent, and gemcitabine, a nucleoside analog—with SUBA™-itraconazole. While traditionally used as an antifungal, itraconazole is repurposed here for its antiangiogenic properties, specifically its ability to inhibit VEGF- and bFGF-mediated pathways, thereby suppressing endothelial cell proliferation and tube formation. The SUBA™ (supersaturated bioavailability) formulation of itraconazole is used to enhance oral absorption. A Phase II trial led by the Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins was initiated to assess this triplet's efficacy but was terminated early due to low patient accrual.
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