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Varenicline (VAR)
Varenicline is a partial agonist at the alpha-4 beta-2 nicotinic acetylcholine receptor that reduces nicotine cravings and blocks the rewarding effects of smoking.
Varenicline is a partial agonist at the alpha-4 beta-2 nicotinic acetylcholine receptor that reduces nicotine cravings and blocks the rewarding effects of smoking. Used for Smoking cessation in adults.
At a glance
| Generic name | Varenicline (VAR) |
|---|---|
| Sponsor | University of Oklahoma |
| Drug class | Nicotinic receptor partial agonist |
| Target | Alpha-4 beta-2 nicotinic acetylcholine receptor |
| Modality | Small molecule |
| Therapeutic area | Addiction/Smoking Cessation |
| Phase | FDA-approved |
Mechanism of action
Varenicline binds with high affinity and selectivity to the alpha-4 beta-2 nicotinic receptor in the brain. As a partial agonist, it provides modest dopamine release to reduce withdrawal symptoms while simultaneously blocking nicotine from binding to and activating the same receptor, thereby diminishing the reinforcing effects of smoking.
Approved indications
- Smoking cessation in adults
Common side effects
- Nausea
- Insomnia
- Abnormal dreams
- Headache
- Dizziness
- Constipation
Key clinical trials
- Trial of Varenicline With Nicotine Lozenges and a Smartphone Medication Adherence Intervention for Smoking Cessation (PHASE2)
- A Smart Approach to Treating Tobacco Use Disorder in Persons Living With HIV (PHASE4)
- Efficacy of Varenicline Tartrate in Treating Frequent Premature Ventricular Contractions (PHASE2)
- Dopamine D2/D3 Receptor Upregulation by Varenicline in Methamphetamine Users (PHASE1)
- Effectiveness of Combination Varenicline and Oral Nicotine Replacement Therapy (COMBO) (PHASE2)
- A Novel Human Lab Model for Screening AUD Medications (PHASE2)
- Individualizing Pharmacotherapy for African American Smokers (PHASE3)
- Combining Varenicline and Naltrexone for Smoking Cessation (PHASE2)
Primary sources
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| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |