Selective relaxant binding agents (SRBAs) are a new class of
drugs that selectively encapsulates and binds
neuromuscular blocking agents (NMBAs). The first drug introduction of an SRBA is
sugammadex. . SRBAs exert a
chelating action that effectively terminates an NMBA ability to bind to
nicotinic receptors.[1]
Examples of SRBAs include:
1. Sugammadex is a modified gamma cyclodextrin that specifically encapsulates and binds the aminosteroid NMBAs: affinity is highest for
rocuronium, followed by
vecuronium, and relatively low affinity for
pancuronium.
2. Adamgammadex is also a modified gamma-cyclodextrin, with acetyl-amino groups replacing the carboxylic acid groups of sugammadex. Early research suggests it may have a lower incidence of adverse reactions than sugammadex [2][3]
3. Calabadion 1 and calabadion 2 are cucurbituril molecules with high binding affinity for both aminosteroid and benzylisoquinoline muscle relaxants.[4] Calabadion 2 has 89 times the affinity for rocuronium than does sugammadex.[5]
Discovery of SRBAs
The discovery of SRBA as a new class of drug is the result of work done by Organon laboratories at the
Newhouse research site in
Scotland.
Cyclodextrins were explored as a means to solubilize rocuronium bromide (a
steroidal NMBA) in a neutral aqueous solution. Upon creating numerous modified cyclodextrins, one particular
molecule was found to possess extremely high affinity for the rocuronium molecule. Originally known as Org25969, it is now generically named sugammadex sodium.
Selective relaxant binding agents (SRBAs) are a new class of
drugs that selectively encapsulates and binds
neuromuscular blocking agents (NMBAs). The first drug introduction of an SRBA is
sugammadex. . SRBAs exert a
chelating action that effectively terminates an NMBA ability to bind to
nicotinic receptors.[1]
Examples of SRBAs include:
1. Sugammadex is a modified gamma cyclodextrin that specifically encapsulates and binds the aminosteroid NMBAs: affinity is highest for
rocuronium, followed by
vecuronium, and relatively low affinity for
pancuronium.
2. Adamgammadex is also a modified gamma-cyclodextrin, with acetyl-amino groups replacing the carboxylic acid groups of sugammadex. Early research suggests it may have a lower incidence of adverse reactions than sugammadex [2][3]
3. Calabadion 1 and calabadion 2 are cucurbituril molecules with high binding affinity for both aminosteroid and benzylisoquinoline muscle relaxants.[4] Calabadion 2 has 89 times the affinity for rocuronium than does sugammadex.[5]
Discovery of SRBAs
The discovery of SRBA as a new class of drug is the result of work done by Organon laboratories at the
Newhouse research site in
Scotland.
Cyclodextrins were explored as a means to solubilize rocuronium bromide (a
steroidal NMBA) in a neutral aqueous solution. Upon creating numerous modified cyclodextrins, one particular
molecule was found to possess extremely high affinity for the rocuronium molecule. Originally known as Org25969, it is now generically named sugammadex sodium.