Drug intelligence / Profile preview

naloxegol

Development stage
Approved
Lead developer
AstraZeneca
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Naloxegol is a peripherally acting μ-opioid receptor antagonist indicated for the treatment of opioid-induced constipation (OIC) in adults with chronic non-cancer pain. It is a PEGylated derivative of α-naloxol, designed to selectively block opioid receptors in the gastrointestinal tract without affecting central analgesia. The pegylation restricts its action to peripheral tissues by preventing significant penetration across the blood-brain barrier. Naloxegol was developed by AstraZeneca and licensed from Nektar Therapeutics. It was approved by the FDA in 2014 for use in adult patients who have been taking opioids for at least four weeks[3][5][1].

Brand names
MovantikMoventig
Other names
PEGylated naloxolα-naloxol PEGylated derivative
02

Targets

MOR (Mu opioid receptor)

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