Drug intelligence / Profile preview

Lusedra

Development stage
Unknown
Lead developer
Eisai
Modality
Small Molecules
Administration
Intravenous
01

Overview

Lusedra (fospropofol disodium) is an intravenous sedative-hypnotic agent developed by Eisai Inc. for monitored anesthesia care (MAC) sedation in adult patients undergoing diagnostic or therapeutic procedures. It is a water-soluble prodrug of propofol, which is released following hydrolysis by alkaline phosphatase enzymes in the body. Once converted, the active metabolite propofol acts as a positive allosteric modulator of GABA-A receptors in the central nervous system, enhancing inhibitory neurotransmission to produce sedation and hypnosis. Lusedra was approved by the FDA in December 2008 and is classified as a Schedule IV controlled substance. Compared to traditional lipid-emulsion propofol, Lusedra offers a different pharmacokinetic profile with a slower onset and longer duration of action, and it does not require the lipid vehicle that can be associated with pain on injection or hyperlipidemia.

Brand names
Lusedra
Other names
fospropofol disodiumfospropofolpropofol phosphate
02

Targets

GABRR (GABA-A receptor subunit rho)

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