sunitinib + ketoconazole

Sunitinib + ketoconazole is a combination of two small molecule drugs used in research and clinical settings to explore enhanced anticancer efficacy and drug-drug interactions. Sunitinib is a multitargeted receptor tyrosine kinase inhibitor that blocks several receptors involved in tumor growth, angiogenesis, and metastasis, including vascular endothelial growth factor receptors (VEGFRs), platelet-derived growth factor receptors (PDGFRs), and c-Kit. Ketoconazole is an antifungal agent that also acts as a potent inhibitor of cytochrome P450 3A4 (CYP3A4), the primary enzyme responsible for metabolizing sunitinib. When combined, ketoconazole increases plasma concentrations of sunitinib by inhibiting its metabolism, which can enhance both efficacy and toxicity. This combination has been studied for its potential to improve anticancer therapy by targeting the tumor microenvironment[1][2][3][5]. However, due to significant pharmacokinetic interactions leading to increased risk of adverse effects from elevated sunitinib levels, this combination should be used with caution or avoided unless therapeutic drug monitoring is available[2][4].