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Drug intelligence / Profile preview
fospropofol disodium (Eisai Co., Ltd.)
- Development stage
- Unknown
- Lead developer
- Eisai
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
Fospropofol disodium is a water-soluble, phosphonooxymethyl prodrug of the intravenous anesthetic propofol. Developed by Eisai (following its acquisition of MGI Pharma), it was approved by the FDA in 2008 under the brand name Lusedra for monitored anesthesia care (MAC) sedation in adult patients undergoing diagnostic or therapeutic procedures. Upon intravenous administration, fospropofol is rapidly converted by endothelial alkaline phosphatases into propofol, phosphate, and formaldehyde. The released propofol then acts as a positive allosteric modulator of the gamma-aminobutyric acid-A (GABA-A) receptor, enhancing the inhibitory effects of GABA in the central nervous system. Unlike the standard lipid emulsion formulation of propofol, fospropofol is an aqueous solution, which significantly reduces pain at the injection site and avoids the complications associated with lipid loads, such as hypertriglyceridemia or risk of microbial growth.
- Brand names
- LusedraAQUAVAN
- Other names
- fospropofol
02
Targets
GABRR (GABA-A receptor subunit rho)
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