Oral Pegylated Naloxol

An orally available formulation containing naloxol, a derivative of the opioid antagonist naloxone, conjugated with polyethylene glycol (PEG), with opioid-induced constipation (OIC)-relieving activity. Upon oral administration, pegylated naloxol binds to and blocks peripheral opioid receptors within the enteric nervous system, thereby preventing constipation induced by opioid receptor activation. Conjugation with PEG prevents penetration through the blood-brain barrier (BBB) and into the central nervous system (CNS), and therefore does not interfere with the analgesic effect of opioids. (NCI Thesaurus)

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