Drug intelligence / Profile preview

fospropofol disodium (MGI Tech)

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

Overview

Fospropofol disodium is a water-soluble phosphate prodrug of the intravenous anesthetic propofol. Upon administration, it is rapidly converted by endothelial alkaline phosphatases into active propofol, phosphate, and formaldehyde. It acts as a positive allosteric modulator of the GABA-A receptor in the central nervous system. Developed to overcome the limitations of propofol lipid emulsions—such as injection pain, risk of fat embolism, and bacterial contamination—fospropofol offers a smoother hemodynamic profile and a more gradual onset of action. It is primarily used for monitored anesthesia care (MAC) sedation in patients undergoing diagnostic or therapeutic procedures and is being investigated for general anesthesia induction and maintenance. In China, it is manufactured by Yichang Humanwell Pharmaceutical and has been the subject of extensive clinical evaluation at institutions like Tongji Hospital.

Brand names
Lusedra
Other names
fospropofolpropofol phosphatefospropofolum natricum
02

Targets

GABRR (GABA-A receptor subunit rho)Glycine receptorNMDAR (Glutamate receptor ionotropic, NMDA)

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