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bupropion + varenicline
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Bupropion + varenicline is a combination of two non-nicotine pharmacotherapies used for smoking cessation. Bupropion is an atypical antidepressant that acts as a norepinephrine-dopamine reuptake inhibitor and also has antagonistic effects on nicotinic acetylcholine receptors. Varenicline is a partial agonist at the α4β2 subtype of neuronal nicotinic acetylcholine receptors, reducing cravings and withdrawal symptoms by partially stimulating these receptors while blocking nicotine binding. The rationale for combining these agents lies in their distinct mechanisms of action, which may provide additive or synergistic effects to improve smoking abstinence rates compared to monotherapy. Clinical trials have shown that the combination can increase prolonged abstinence rates in certain populations, particularly among male smokers and those with high nicotine dependence[1][2][3][5]. Both drugs are generally well tolerated but carry risks such as neuropsychiatric side effects.
- Other names
- bupropion SR + vareniclinebupropion sustained-release + varenicline
02
Targets
CHRNA7 (α7 nicotinic receptor)α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)DAT (Dopamine plasma membrane transport protein)α3β2 nAChR (α3β2 nicotinic receptor)NET (Norepinephrine Transporter)
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