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nicotine + bupropion + varenicline

Development stage: Preclinical
Lead developer: GSK
Modality: Small Molecules
Administration: Oral, Transdermal, Sublingual, Intranasal, Inhalation

Overview

A combination therapy approach for smoking cessation that utilizes three different FDA-approved smoking cessation medications: nicotine replacement therapy, bupropion sustained-release (SR), and varenicline. Each medication works through different mechanisms to help reduce nicotine cravings and withdrawal symptoms. Varenicline acts as a partial agonist at α4β2 neuronal nicotinic acetylcholine receptors, bupropion works through noradrenergic and dopaminergic systems, and nicotine replacement therapy provides controlled doses of nicotine to reduce withdrawal symptoms.

Targets

CHRNA7 (α7 nicotinic receptor)α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)α3β4 nAChR (α3β4 nicotinic receptor)DAT (Sodium-dependent dopamine transporter)NET (Sodium-dependent noradrenaline transporter)

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