10230. Sugammadex

Nomenclature

CAS number: 343306-71-8
6A,6B,6C,6D,6E,6F,6G,6H-Octakis-S-(2-carboxyethyl)-6A,6B,6C,6D,6E,6F,6G,6H-octathio-γ-cyclodextrin; 6-perdeoxy-6-per(2-carboxyethyl)thio-γ-cyclodextrin.
C72H112O48S8; mol wt 2002.15.
C 43.19%, H 5.64%, O 38.36%, S 12.81%.

Description and references

Selective relaxant binding agent (SRBA). Cyclodextrin-based host molecule that reverses the action of steroidal neuromuscular blocking drugs via selective binding and encapsulation. Prepn: M. Zhang et al., WO 0140316; eidem, US 6670340 (2001, 2003 both to Akzo Nobel). Synthesis, structure-activity, and x-ray crystallography: J. M. Adam et al., J. Med. Chem. 45, 1806 (2002) DOI PubMed. Crystal structure of complex with rocuronium: A. Bom et al., Angew. Chem. Int. Ed. 41, 266 (2002) DOI. LC/MS determn in plasma and urine: O. Epemolu et al., Rapid Commun. Mass Spectrom. 16, 1946 (2002) DOI PubMed. Clinical pharmacokinetics and safety assessment: F. Gijsenbergh et al., Anesthesiology 103, 695 (2005) DOI PubMed. Series of articles on pharmacology and clinical experience: Anesth. Analg. 104, 555-586 (2007) DOI PubMed.

Chemical structure

Derivative

Octasodium salt.

Nomenclature

CAS number: 343306-79-6
Sugammadex sodium; Org-25969.
C72H104Na8O48S8; mol wt 2178.01.
C 39.70%, H 4.81%, Na 8.44%, O 35.26%, S 11.78%.

Properties

Colorless, orthorhombic crystals from DMF + water. d 1.446. Sol in water.

Therapeutic Category

Reversal agent for neuromuscular blocking drugs.

Keywords

Neuromuscular Block Reversant