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fospropofol sodium
- Development stage
- Unknown
- Lead developer
- Eisai
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
Fospropofol sodium is a water-soluble, phosphate ester prodrug of the intravenous anesthetic agent propofol. Upon intravenous administration, it is rapidly hydrolyzed by endothelial alkaline phosphatases to release active propofol, formaldehyde, and phosphate. The liberated propofol acts as a positive allosteric modulator of the $\gamma$-aminobutyric acid type A (GABA-A) receptor, enhancing the inhibitory effects of GABA and leading to sedation or general anesthesia. Developed by MGI Pharma (later acquired by Eisai), fospropofol sodium was designed to overcome the limitations of the standard propofol lipid emulsion, such as pain on injection, risk of fat embolism, and potential for microbial growth. It is primarily indicated for monitored anesthesia care (MAC) sedation in adult patients undergoing diagnostic or therapeutic procedures.
- Brand names
- Lusedra
- Other names
- fospropofol disodiumAquavanfospropofol
02
Targets
NMDAR (Glutamate receptor ionotropic, NMDA)GABRR (GABA-A receptor subunit rho)TNAP (Tissue-nonspecific alkaline phosphatase)Nicotinic Acetylcholine Receptor
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