Drug intelligence / Profile preview

nalbuphine + naloxone

Development stage
Preclinical
Lead developer
Trevi Therapeutics
Modality
Small Molecules
Administration
Intravenous, Intramuscular, Intranasal
01

Overview

Nalbuphine + naloxone is an experimental fixed-ratio combination of the kappa-opioid agonist nalbuphine and the opioid antagonist naloxone. The combination has been studied in a 12.5:1 ratio for management of pain, particularly in post-surgical settings. Nalbuphine acts as a moderate-efficacy partial agonist/antagonist at μ-opioid receptors and a high-efficacy partial agonist at κ-opioid receptors, while naloxone is a pure opioid antagonist. This combination may provide effective analgesia while potentially reducing side effects associated with pure opioid agonists. Recent research also suggests nalbuphine may potentiate naloxone's ability to reverse fentanyl overdose.

02

Targets

KOR (Kappa opioid receptor)MOR (Mu opioid receptor)DOR (Opioid Receptor Delta 1)

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