Drug intelligence / Profile preview

propofol hemisuccinate

Development stage
Preclinical
Lead developer
Epalex
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral, Inhalation (investigational)
01

Overview

Propofol hemisuccinate is a water-soluble prodrug of propofol, designed to improve the oral and parenteral bioavailability of the parent drug. Upon administration, it is rapidly de-esterified in vivo to release active propofol. Propofol acts primarily as a positive allosteric modulator and agonist at GABA-A receptors in the central nervous system, enhancing inhibitory neurotransmission and producing sedative-hypnotic effects. Propofol also possesses antioxidant properties due to its phenolic structure. Propofol hemisuccinate has been investigated for use in migraine and acute repetitive seizures (including epilepsy), with preclinical evidence supporting antiseizure activity after oral administration. It has also shown efficacy in animal models of autoimmune encephalomyelitis by reducing inflammation and oxidative stress[4][5][8].

Brand names
Epalex
Other names
succinic acid monopropofol esterbutanedioic acid, 1-(2,6-bis(1-methylethyl)phenyl) ester
02

Targets

GABRR (GABA-A receptor subunit rho)

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