Neuromuscular blocker binders around the corner?
Posted by Clark Venable on 5/19/2005
Organon is working on the first of a new class of drugs called selective relaxant binding agents (SRBA). The first drug, called Org 25969, is about to enter phase three trials in the US. These drugs can supposedly reverse neuromuscular blockade at any depth of neuromuscular block by binding the neuromuscular blocker.
Though this news release and the Organon website are short on details, this site has the scoop:
"The novel concept of using a ring-shaped cyclodextrin to engulf a neuromuscular blocking drug is fascinating.2 Cyclodextrins are cyclic oligosaccharides which are recognised to encapsulate lipophilic molecules such as steroids. They are water soluble and well tolerated biologically. Org 25969 consists of eight such sugar molecules in a ring, the outside of which is hydrophilic, and the inside, hydrophobic. The size and shape of the ring is designed to produce a cavity into which a neuromuscular blocking drug such as rocuronium will tightly fit. Org 25969 is capable of forming a binary host – guest complex of high affinity with rocuronium, for two of its externally charged side-chains react with the quaternary nitrogen groups of the muscle relaxant. It is able to encapsulate all four steroidal rings of rocuronium within its lipophilic cavity. This encapsulation or chelation reverses the effect of rocuronium, by preventing its access to the nicotinic receptor and promoting its dissociation from it."
[via Medical News Today]
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