New drug sugammadex: a selective relaxant binding agent.
Cyclodextrins are molecules with a hollow, truncated cone shape that possess unique lipophilic and hydrophilic properties. These unique properties enable cyclodextrins to engulf and bind lipophilic molecules while maintaining aqueous solubility. Encapsulation of molecules is the principal action of a new drug class, selective relaxant binding agents, which binds and inactivate aminosteroid nondepolarizing muscle relaxants. Sugammadex is the name of a modified cyclodextrin currently in phase 3 studies by Organon International (Oss, The Netherlands), and it may hold promise for a new concept in muscle relaxant reversal. Encapsulation rather than competitive antagonism of neuromuscular blockade may be a future modality of anesthetic practice.
Welliver
Mark
M
University of Florida & Shands Health Science Center, Jacksonville, USA. mark.welliver@gmail.com
D000732:Androstanols / Q000037:antagonists & inhibitors; D000758:Anesthesia / Q000379:methods / Q000639:trends; D000818:Animals; D001667:Binding, Competitive; D002415:Cats; D002626:Chemistry, Pharmaceutical; D002986:Clinical Trials as Topic; D004337:Drug Carriers; D004341:Drug Evaluation; D005544:Forecasting; D006168:Guinea Pigs; D000882:Haplorhini; D006801:Humans; D008657:Metabolic Clearance Rate; D051379:Mice; D003473:Neuromuscular Nondepolarizing Agents / Q000037:antagonists & inhibitors; D000077123:Rocuronium; D012995:Solubility; D000077122:Sugammadex; D047408:gamma-Cyclodextrins / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*
D000732:Androstanols; D004337:Drug Carriers; D003473:Neuromuscular Nondepolarizing Agents; D047408:gamma-Cyclodextrins; D000077122:Sugammadex; D000077123:Rocuronium