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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.
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