Drug intelligence / Profile preview

thienorphine

Development stage
Phase 2
Lead developer
Beijing Institute of Pharmacology and Toxicology
Modality
Small Molecules
Administration
Oral, Subcutaneous
01

Overview

Thienorphine is a potent, long-acting, orally-active **partial agonist** of opioid receptors, structurally related to buprenorphine, developed by the Beijing Institute of Pharmacology and Toxicology as a potential treatment for opioid dependence and addiction. It displays high affinity and balanced binding to the μ-opioid, κ-opioid, and δ-opioid receptors, acting as a partial agonist at μ- and κ-opioid receptors and as an antagonist at δ-opioid receptors. Thienorphine has greater oral bioavailability and a longer duration of action compared to buprenorphine. It exhibits lower physical and psychological dependence liability than buprenorphine in preclinical models and is in Phase II clinical development for opioid addiction and relapse prevention[1][3][4][5][7][9].

Other names
thienorphine
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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