OBJECTIVE： To establish a method for the determination of dasatinib concentration in human plasma and study the bioequivalence of 2 kinds of tablets. METHODS： In a randomized two-way crossover study， 24 healthy male volunteers were divided into two groups， and were administered respectively with test and reference preparations 100 mg under fasting and fed conditions. The plasma concentration of dasatinib was determined by LC-MS/MS. Using imatinib mesylate as internal standard， the determination was performed on Welchrom C18 column with mobile phase consisted of acetonitrile-0.1％ formic acid （70 ∶ 30， V/V）. Positive ion scanning was conducted under MRM mode， ESI， and ion pair for quantitative analysis were m/z 488.5→401.2 （dasatinib） and m/z 494.6→394.2 （internal standard）. DAS 3.2.8 software was used for data processing and variance analysis was adopted to investigate the bioequivalence of 2 kinds of tablets. RESULTS： The linear rang of dasatinib was 1-300 ng/ml. The pharmacokinetic parameters of test and reference preparations under fasting conditions were as follows： cmax were （165.599±67.592） and （164.533±77.960） ng/ml； tmax were （1.145±0.504） and （1.080±0.467） h； t1/2 were （5.080±2.262） and （3.771±1.596） h； AUC0-36 h were （550.487±256.494） and （585.986±324.885） ng·h/ml. The pharmacokinetic parameters of test and reference preparations under fed conditions were as follows： cmax were （163.058±47.533） and （165.440±53.012） ng/ml； tmax were （1.630±1.066） and （1.576±0.530） h； t1/2 were （4.720±2.677） and （4.311±2.610） h； AUC0-36 h were （568.036±192.521） and （601.100±216.855） ng·h/ml. Relative bioavailability of AUC0-36 h under fasting and fed conditions were （100.2±7.5）％ and （99.2±3.8）％. Analysis of variance showed there were no significant difference in the pharmacokinetic parameters of between 2 preparations and cyde （P＞0.05）， there was statistical significance among subjects （P＜0.05）. CONCLUSIONS： LC-MS/MS method can determine the concentration of dasatinib in human plasma rapidly； and the two preparations are bioequivalent.