Drug intelligence / Profile preview

6-beta-naltrexol-hydroxybupropion codrug

Development stage
Preclinical
Lead developer
University of Kentucky
Modality
Small Molecules
Administration
Transdermal
01

Overview

CB-NTXOL-BUPOH is a transdermal codrug composed of 6-beta-naltrexol and hydroxybupropion, linked via a carbonate bond. 6-beta-naltrexol is the primary active metabolite of naltrexone and serves as a potent mu-opioid receptor antagonist, while hydroxybupropion is an active metabolite of bupropion that acts as a norepinephrine-dopamine reuptake inhibitor (NDRI) and a nicotinic acetylcholine receptor antagonist. The codrug is designed to improve the percutaneous absorption of these agents for the simultaneous treatment of alcohol dependence and tobacco addiction. By utilizing a transdermal delivery system, the formulation aims to provide steady-state plasma concentrations, reduce first-pass metabolism, and improve patient compliance in treating comorbid substance use disorders.

Other names
6-beta-naltrexol-hydroxybupropion codrug6-beta-naltrexol hydroxybupropion carbonate codrugCB-NTXOL-BUPOH
02

Targets

DAT (Dopamine plasma membrane transport protein)MOR (Mu opioid receptor)NET (Norepinephrine Transporter)Nicotinic Acetylcholine Receptor

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