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Varenicline Pill
Varenicline is a partial agonist at the alpha-4 beta-2 nicotinic acetylcholine receptor that reduces nicotine cravings and blocks the rewarding effects of nicotine.
Varenicline is a partial agonist at the alpha-4 beta-2 nicotinic acetylcholine receptor that reduces nicotine cravings and blocks the rewarding effects of nicotine. Used for Smoking cessation in adults.
At a glance
| Generic name | Varenicline Pill |
|---|---|
| Also known as | Chantix, Varenicline |
| Sponsor | National Institute on Drug Abuse (NIDA) |
| 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 subtype in the brain. As a partial agonist, it provides modest dopamine release to reduce withdrawal symptoms while simultaneously blocking nicotine from binding to these receptors, thereby diminishing the reinforcing effects of smoking and reducing the motivation to use tobacco.
Approved indications
- Smoking cessation in adults
Common side effects
- Nausea
- Insomnia
- Abnormal dreams
- Headache
- Dizziness
- Constipation
- Flatulence
Key clinical trials
- Advancing VR-based Attentional Bias as a Biomarker for Tobacco Use Disorder (EARLY_PHASE1)
- Combination Nicotine Replacement Therapy, Cytisine, or Varenicline for Smoking Cessation (PHASE4)
- STARS (Smoking Treatment And Remote Sampling) Study (PHASE1, PHASE2)
- Reward Sensitivity and Pharmacotherapy for Smoking Cessation (PHASE4)
- Switching to E-cigarettes in Smokers Not Interested in Quitting (PHASE3)
- The Avenues Study: Dual Use Cessation (PHASE4)
- Health Systems Reach Interventions Project (PHASE4)
- Cessation Screening Project (PHASE4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Varenicline Pill CI brief — competitive landscape report
- Varenicline Pill updates RSS · CI watch RSS
- National Institute on Drug Abuse (NIDA) portfolio CI