naloxol

Naloxol is a small molecule opioid antagonist and a primary human metabolite of naloxone, formed via the enzymatic reduction of naloxone's 6-keto group. It exists as two diastereomers, alpha-naloxol and beta-naloxol. While naloxol exhibits antagonist activity at mu-opioid receptors, it is not developed or marketed as a standalone therapeutic agent. Its clinical relevance primarily stems from its role as a metabolite and its use as the structural precursor for naloxegol, a PEGylated derivative of alpha-naloxol. Naloxegol is designed to be peripherally selective, treating opioid-induced constipation without compromising central analgesia, a property achieved by the PEGylation of the naloxol scaffold which restricts blood-brain barrier penetration.

Other names

alpha-naloxolbeta-naloxol6-alpha-naloxol6-beta-naloxol6-hydroxynaloxoneN-allylnormorphine-6-olN-allylnormorphine6-olN-allylnormorphine 6-ol