Last reviewed · How we verify

Standard Duration Varenicline

University of Wisconsin, Madison · 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 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.

At a glance

Generic nameStandard Duration Varenicline
SponsorUniversity of Wisconsin, Madison
Drug classNicotinic receptor partial agonist
TargetAlpha-4 beta-2 nicotinic acetylcholine receptor
ModalitySmall molecule
Therapeutic areaAddiction/Smoking Cessation
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 the same receptor, preventing the reinforcing effects of smoking. This dual action makes it effective for smoking cessation.

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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