pazopanib + ketoconazole

**Pazopanib + ketoconazole** is a non-fixed drug combination used clinically for pharmacokinetic interaction studies rather than as a marketed pharmaceutical product. **Pazopanib** is an oral small molecule multikinase inhibitor targeting vascular endothelial growth factor receptors (VEGFR)-1, -2, and -3, platelet-derived growth factor receptors (PDGFR)-α and -β, fibroblast growth factor receptor (FGFR), and c-Kit; it is approved for use in renal cell carcinoma and soft tissue sarcoma. **Ketoconazole** is a strong inhibitor of cytochrome P450 3A4 (CYP3A4) and is primarily an antifungal agent. When coadministered, ketoconazole significantly increases the systemic exposure of pazopanib due to inhibition of its metabolism by CYP3A4, resulting in a 1.66-fold increase in area under the curve (AUC) and 1.45-fold increase in maximum plasma concentration (Cmax). Coadministration is generally not recommended; if necessary, the dose of pazopanib should be halved to minimize toxicity. The combination is not a marketed therapy but may be encountered in drug-interaction or dose-adjustment contexts[1][2].

Other names

pazopanib + ketoconazole