Naloxegol is a peripherally-selective opioid antagonist used to treat opioid-induced constipation (OIC) in adult patients with chronic non-cancer pain. The advantage of naloxegol over the opioid antagonist naloxone is that its PEGylated structure allows for high selectivity for peripheral opioid receptors and lack of entry into the central nervous system through the blood-brain barrier.
- Mechanism
- Curator reviewed
Naloxegol is an antagonist of opioid binding at the mu-opioid receptor. When administered at the recommended dose levels, naloxegol functions as a peripherally-acting mu-opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids. Naloxegol has shown more than 6000 fold selectivity for the peripheral mu receptors, and its PEGylated form restricts its action only to the periphery, not affecting the pain-relieving mechanism of opioids in the central nervous system.
- Primary indication
- Indicated for the treatment of opioid-induced constipation (OIC) in adult patients with chronic non-cancer pain.Curator reviewed · 1 structured indication
- Formula / weight
- C34H53NO11 · 651.794 g/mol (avg)
- First approval
- Canada, 2017 · United States, 2015 · European Union, 2016
- Code names
- AZ-13337019 · NKTR-118
- Brand names
Resolves to
XNKCCCKFOQNXKV-ZRSCBOBOSA-NSMILESCOCCOCCOCCOCCOCCOCCOCCO[C@H]1CC[C@@]2(O)[C@H]3CC4=CC=C(O)C5=C4[C@@]2(CCN3CC=C)[C@H]1O5What you can answer from here — as of September 23, 2026
Which drugs share a target with Naloxegol, and which of those have an active Phase 3 trial?
Create a free account or log in to explore the full data card.
Create Account