Drug intelligence / Profile preview

gantacurium

Development stage
Phase 2
Lead developer
Merck
Modality
Small Molecules
Administration
Intravenous
01

Overview

Gantacurium is an investigational, ultra-short acting, non-depolarizing neuromuscular blocking agent of the asymmetric mixed-onium chlorofumarate class. It is a single-isomer isoquinolinium diester of chlorofumaric acid and represents a third-generation tetrahydroisoquinolinium (THIQ) neuromuscular blocker. Gantacurium acts as an antagonist at the neuronal acetylcholine receptor subunit alpha-3, thereby inhibiting neuromuscular transmission and inducing skeletal muscle relaxation. Its onset is rapid and its duration of action is comparable to succinylcholine but without the latter’s side effects. Gantacurium undergoes unique metabolism via rapid cysteine adduction (chemo-inactivation) and slower pH-sensitive hydrolysis, allowing for spontaneous or l-cysteine-induced reversal of blockade[1][2][3][4][5].

Other names
gantacurium chloride
02

Targets

CHRNA3 (nAChR α3 subunit)

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