Department of Anesthesiology

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Novel neuromuscular blocking drugs and antagonists.

TitleNovel neuromuscular blocking drugs and antagonists.
Publication TypeJournal Article
Year of Publication2015
AuthorsHeerdt PM, Sunaga H, Savarese JJ
JournalCurr Opin Anaesthesiol
Volume28
Issue4
Pagination403-10
Date Published2015 Aug
ISSN1473-6500
Abstract

PURPOSE OF REVIEW: This review summarizes recent progress in the development of new muscle relaxants that are inactivated by cysteine, and considers the evolving paradigm of selective relaxant binding or degrading agents that can reverse neuromuscular blockade at any time.

RECENT FINDINGS: The benzylisoquinoline compound gantacurium is a nondepolarizing muscle relaxant with an ultrashort duration largely determined by the rapid rate at which endogenous L-cysteine binds to, and permanently inactivates, the molecule. Although the clinical development of gantacurium has been hampered by modest histamine release, preclinical studies demonstrating that the drug can be rapidly reversed by injecting L-cysteine led to the development of CW002, an intermediate duration molecule that can also be reversed at any time by L-cysteine injection. Clinical trials with CW002 are now underway. The ability to reverse complete paralysis with cysteine dovetails with the established selective aminosteroid binding agent sugammadex, and the recently described universal relaxant binding agent calabadion. Taken together, the concept of rapid reversal at any time raises the question of whether an ultrashort nondepolarizing drug is needed if safe and cost-effective relaxant binding agents are available.

SUMMARY: The gantacurium derivative CW002 is an intermediate duration, nondepolarizing, cysteine-inactivated, neuromuscular blocking drug currently in clinical trials. Like sugammadex reversal of rocuronium, CW002 can be reversed at any time by cysteine injection.

DOI10.1097/ACO.0000000000000209
Alternate JournalCurr Opin Anaesthesiol
PubMed ID26087274