AIM: To study the pharmacokinetics (PK) of pazopanib tablets and explore the genetic mechanism of individual differences in drug metabolism primarily. METHODS: Fourteen healthy male subjects were respectively administrated with a single dose pazopanib tablet (200 mg) orally on the day of dosing, and their blood samples were collected from baseline to 96 hours. The serum concentration of pazopanib was measured by LC-MS/MS, the parameters of PK were calculated by winnonlin 6.3 software, and the gene polymorphism of cytochrome P450 3A4 (CYP3A4) was determined by snapshot method. RESULTS: The range of C