Drug intelligence / Profile preview

moxetomidate

Development stage
Phase 3
Lead developer
Novartis
Modality
Small Molecules
Administration
Intravenous
01

Overview

Moxetomidate (also known as ABP-700) is an intravenous anesthetic and a second-generation derivative of etomidate. It was designed as a "soft drug" to retain the potent sedative properties and hemodynamic stability of etomidate while overcoming its most significant drawback: the prolonged adrenocortical suppression caused by the inhibition of 11β-hydroxylase. Moxetomidate achieves this through the incorporation of a methoxycarbonyl ester group that is rapidly hydrolyzed by non-specific tissue esterases into an inactive carboxylic acid metabolite. This metabolic pathway results in a drug with an ultra-short duration of action and a rapid, predictable recovery profile, making it a candidate for continuous infusion during general anesthesia and procedural sedation. Despite its promising pharmacokinetic profile, clinical development was hindered by the observation of excitatory phenomena, such as involuntary muscle movements, in clinical trials.

Other names
methoxycarbonyl-etomidate
02

Targets

GABRR (GABA-A receptor subunit rho)

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