Pharmacokinetics of Sugammadex: An Open‐Label, 3‐Period, Fixed‐Sequence, 3‐Single‐Doses Study in Healthy Chinese Subjects

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.