Discovery, development, and clinical application of sugammadex sodium, a selective relaxant binding agent

Mark Welliver^1,3, John McDonough^1,3, Nicholas Kalynych^1,2,3, Robert Redfern³

¹University of North Florida, Nurse Anesthetist Program, Jacksonville, Florida, USA; ²Shands Jacksonville, Perioperative Services, Jacksonville, Florida, USA; ³University of Florida, Department of Anesthesiology, Jacksonville, Florida, USA

Abstract: Neuromuscular blockade, induced by neuromuscular blocking agents, has allowed prescribed immobility, improved surgical exposure, optimal airway management conditions, and facilitated mechanical ventilation. However, termination of the effects of neuromuscular blocking agents has, until now, remained limited. A novel cyclodextrin encapsulation process offers improved termination of the paralytic effects of aminosteroidal non-depolarizing neuromuscular blocking agents. Sugammadex sodium is the first in a new class of drug called selective relaxant binding agents. Currently, in clinical trials, sugammadex, a modified gamma cyclodextrin, has shown consistent and rapid termination of neuromuscular blockade with few side effects. The pharmacology of cyclodextrins in general and sugammadex in particular, together with the results of current clinical research are reviewed. The ability of sugammadex to terminate the action of neuromuscular blocking agents by direct encapsulation is compared to the indirect competitive antagonism of their effects by cholinesterase inhibitors. Also discussed are the clinical implications that extend beyond fast, effective reversal, including numerous potential peri-operative benefits.

Keywords: modified cyclodextrin, selective relaxant binding agent (SRBA), sugammadex, encapsulation, muscle relaxants, neuromuscular blockade reversal