Drug intelligence / Profile preview

Buprenorphine + norbuprenorphine

Development stage
Unknown
Lead developer
Reckitt
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Sublingual, Transdermal, Intravenous, Intramuscular, Subcutaneous, Buccal, Epidural, Intrathecal
01

Overview

Buprenorphine + norbuprenorphine refers to the presence of both buprenorphine, a semi-synthetic opioid, and its major active metabolite, norbuprenorphine. Buprenorphine is primarily used for opioid use disorder and pain management. It acts as a partial agonist at the mu-opioid receptor, an antagonist at the kappa-opioid receptor, and an agonist at the nociceptin receptor. This unique pharmacology results in effective suppression of withdrawal symptoms with a lower risk of respiratory depression compared to full agonists[5][6][8]. Norbuprenorphine is formed via N-dealkylation by CYP3A4 metabolism of buprenorphine and is itself an active metabolite. Unlike buprenorphine, norbuprenorphine is a full agonist at mu-, delta-, and nociceptin receptors but has much less antinociceptive potency while causing more pronounced respiratory depression due to poor brain penetration[1][6][8]. Both compounds are further glucuronidated before excretion.

02

Targets

KOR (Kappa opioid receptor)NOP (Nociceptin/orphanin FQ peptide receptor)MOR (Mu opioid receptor)DOR (Opioid Receptor Delta 1)

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