The main purpose of this study was to assess pharmacokinetic parameters (area under the plasma concentration–time curve from time 0 to infinity, area under the plasma concentration–time curve from time 0 to the last measurable concentration, maximum concentration, and apparent terminal half-life) after administration of 3 single intravenous (IV) doses of sugammadex to evaluate the safety and tolerability in healthy nonanesthetized subjects. This was an open-label, 3-period, nonrandomized, single-rising-dose study in 12 healthy Chinese subjects 18 to 45 years of age. In each period, every subject received a single IV dose of sugammadex in a fixed sequence (1, 2, and 4 mg/kg) under fasting conditions. There was a 3-day washout phase between dosing in each treatment period. In this study, a total of 11 (6 men and 5 women) Chinese subjects (with mean age of 25 ± 4.0 years; body weight, 64 ± 6 kg; height, 167 ± 6 cm; and body mass index, 22.9 ±1.2 kg/m2) received single doses of sugammadex 1, 2, and 4 mg/kg sequentially, with a 3-day washout phase between consecutive doses, and completed the study. The geometric mean maximum concentrations were 16.81, 30.99, and 60.55 μg/mL for sugammadex 1, 2, and 4 mg/kg, respectively. The median time to maximum concentration was 0.03 hour after bolus administration, and plasma sugammadex concentrations declined with a mean apparent terminal half-life of ≈1.7 hours across all 3 doses. Single-dose IV administration of sugammadex 1, 2, and 4 mg/kg was generally safe and well tolerated in healthy Chinese male and female subjects.