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Varinecline (Chantix)

American University of Beirut Medical Center · FDA-approved active Small molecule

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.

At a glance

Generic nameVarinecline (Chantix)
SponsorAmerican University of Beirut Medical Center
Drug classNicotinic receptor partial agonist
TargetAlpha-4 beta-2 nicotinic acetylcholine receptor
ModalitySmall molecule
Therapeutic areaPsychiatry / Addiction Medicine
PhaseFDA-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 these receptors, preventing the reinforcing effects of smoking and reducing the urge to smoke.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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