OBJECTIVE：To establish the method for the simultaneous determination of clopidogrel（CLO）and its active metabolites（CATM）and inactive metabolites（CCAM），and to conduct pharmacokinetic study. METHODS：The plasma sample had been derivatized by 2-bromine-3′ -methoxy acetophenone（MPB），and was precipitated by acetonitrile. Using carbamazepine as internal standard，UPLC-MS/MS was adopted. The separation was performed on Waters ACQUITY UPLC HSS T3 column with mobile phase consisted of water（containing 0.1％ formic acid）-acetonitrile（containing 0.1％ formic acid）using a gradient elution program at the flow rate of 0.50 ml/min. The ESI was equipped and quantitative analysis was operated in positive ion and MRM mode. The mass transition ion-pairs were followed as m/z 322.1→211.8（CLO），m/z 504.1→155.0（the alkylation derivatives of CATM，CATMD），m/z 308.3→198.0（CCAM），m/z 273.2→194.3（internal standard）. RESULTS：The linear calibration curves for CLO，CATMD and CCAM were obtained in the concentration range of 0.03-20.00 ng/ml，0.30-200.00 ng/ml and 10.00-10 000.00 ng/ml in plasma，respectively；intra-day and inter-day RSD for them were all less than 15％，and relative error（RE）ranged from －3.5％ to 5.7％. Main pharmacokinetic parameters of CLO，CATMD and CCAM in 5 healthy volunteers after oral administration of CLO 300 mg were as follows：cmax were（7.89±5.46），（15.58±8.08），（8 023.33± 1 047.39）ng/ml；tmax were（1.25±0.43），（1.25±0.43），（1.67±0.29）h；t1/2 were（2.31±0.61），（0.64±0.08），（6.53±2.55）h； AUC0-t were（17.19±14.59），（21.39±9.58），（30 648.85±8 026.63）ng·h/ml. CONCLUSIONS：The established method is sensitive， rapid and convenient，which is suitable for pharmacokinetic study and plasma concentration determination of CLO and its metabolites.