Sugammadex (SUG), fast reversal of neuromuscular blockade, is a novel antagonist of neuromuscular blocking agents (NMBA). Rocuronium, one of NMBAs, is usually used to get better surgical conditions in kidney transplant surgeries. Nevertheless, rocuronium has lots of shortages, such as increasing risk of pulmonary complications. Thus, SUG is vital to kidney transplant surgery. However, because SUG is excreted by the kidneys in prototypes, the pharmacokinetics (PK) may be affected in patients with renal impairment. A liquid chromatography tandem mass spectrometry (LC-MS/MS) method was developed to monitor the SUG plasma samples to investigate the PK of SUG in kidney transplant patients. Due to the complexity and limitation of other sample preparation methods, magnetic solid phase extraction (MSPE）was adopted to purify samples. The chromatographic separation was obtained by using a reverse Polaris C18 column and gradient elution with 0.1% formic acid (FA) in water as phase A and in methanol (MeOH) as phase B as mobile phases. The transitions 999.7→963.9 (m/z) and 1055.7→1012.2 (m/z) were used to quantify of SUG and ORG26265 separately under the negative electrospray ionization mode. Linear calibration curve was achieved in the concentration varying from 100 to 10000 ng/ml. The acceptable accuracy varied from 95.72% to 106.42% and intra- and inter-precision did not exceed 15% (20% at the lower limit of quantitation (LLOQ)). Matrix effect, stability, dilution integrity, and carry-over have all been validated. This method was successfully applied for the pharmacokinetic study of 13 recipients and 12 donors of kidney transplant after the intravenous injection of 2 mL/kg SUG.