Abstract: OBJECTIVE To establish an LC-MS method for the determination of pitavastatin in the human plasma. METHODS Pitavastatin and internal standard (IS, rosuvastatin) were separated on a Shim-pack C18 column. The mobile phase consisted of methanol/water (A/B) with 0.025% aqueous ammonia and 0.05 mmol·L^-1 ammonium acetate. Gradient elution mode was established. The samples were extracted with ethyl acetate and determined by LC-MS with selected ion monitoring (SIM) mode. RESULTS The linear calibration curve was obtained in the concentration range of 0.2-200.0 ng·mL^-1 (r=0. 999 9), the average extraction recovery was 86.28% and the RSD of inter- and intra-day were less than 12%. CONCLUSION　The developed analytical method was proved accurate, rapid, convenient, and suitable for the determination of pitavastatin in the human plasma and pharmacokinetic studies of pitavastatin.