Oliceridine for pain

A recent study reports that oliceridine, an opioid drug, has fewer adverse effects compared with morphine for postoperative pain relief.

Oliceridine is an opioid drug that is used intravenously for severe acute pain.  It is a G-protein, μ-opioid receptor biased agonist developed by Trevena.  A study published in The Journal of Pain Research found that an IV of oliceridine was generally safe and well tolerated for management of moderate to severe pain.  The study was called ATHENA and examines the safety and effectiveness of oliceridine.  A total of 768 people received oliceridine.  The mean age was 54.1 years with most participants being caucasian females.  Most participants were surgical patients at 94%.

Oliceridine has fewer adverse effects than other opioid drugs

Many patients require opioid therapy and oliceridine is a promising opioid drug as it is similar to morphine but with fewer adverse effects.  Oliceridine is a G-protein selective analgesic that has less recruitment of βarrestin than morphine or fentanyl.  β-arrestin is a signalling pathway associated with opioid-related adverse events especially when activated simultaneously with G-protein pathways.  G-protein pathway leads to analgesia while the β-arrestin pathway leads to adverse effects.  Other opioids are not selective and activate both pathways.  So while you get the benefit of analgesia it comes at the expense of safety and tolerability.  Oliceridine is selective and biased towards the G-protein signalling pathway.

The study reported adverse events in 64% of participants.  Only two percent had a severe reaction while 37% had a mild reaction and 25% had a moderate reaction to oliceridine.  The most frequent reaction to oliceridine was nausea, at 31%, followed by constipation, at 11%.  Higher doses of oliceridine were associated with a greater incidence of adverse side effects

The study found oliceridine to be effective inducing a rapid reduction in pain intensity.  No deaths or cardiorespiratory events were reported.


Written by Katrina F. Zafer, BSc



  1. Bergese, S.D., Brzezinski, M., Hammer, G.B., Beard, T.L., Pan, P.H., Mace, S.E., Berkowitz, R.D., Cochrane, K., Wase, L., Minkowitz, H.S., Habib, A.S. (2019) ATHENA: A Phase 3, Open-Label Study of the Safety and Effectiveness of Oliceridine (TRV130), A G-protein Selective Agonist At the μ-Opioid Receptor, in Patients with Moderate to Severe Acute Pain Requiring Parenteral Opioid Therapy. The Journal of Pain Research.

Image by Arek Socha from Pixabay

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