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Varenicline (Champix)

University of British Columbia · FDA-approved active Small molecule

Varenicline (Champix) is a Nicotinic receptor partial agonist Small molecule drug developed by University of British Columbia. It is currently FDA-approved for Smoking cessation in adults.

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 nameVarenicline (Champix)
SponsorUniversity of British Columbia
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 subtype 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 these receptors, thereby diminishing the reinforcing effects of smoking.

Approved indications

Common side effects

Key clinical trials

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

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

Competitive intelligence

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Frequently asked questions about Varenicline (Champix)

What is Varenicline (Champix)?

Varenicline (Champix) is a Nicotinic receptor partial agonist drug developed by University of British Columbia, indicated for Smoking cessation in adults.

How does Varenicline (Champix) work?

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.

What is Varenicline (Champix) used for?

Varenicline (Champix) is indicated for Smoking cessation in adults.

Who makes Varenicline (Champix)?

Varenicline (Champix) is developed and marketed by University of British Columbia (see full University of British Columbia pipeline at /company/university-of-british-columbia).

What drug class is Varenicline (Champix) in?

Varenicline (Champix) belongs to the Nicotinic receptor partial agonist class. See all Nicotinic receptor partial agonist drugs at /class/nicotinic-receptor-partial-agonist.

What development phase is Varenicline (Champix) in?

Varenicline (Champix) is FDA-approved (marketed).

What are the side effects of Varenicline (Champix)?

Common side effects of Varenicline (Champix) include Nausea, Insomnia, Abnormal dreams, Headache, Dizziness, Constipation.

What does Varenicline (Champix) target?

Varenicline (Champix) targets Alpha-4 beta-2 nicotinic acetylcholine receptor and is a Nicotinic receptor partial agonist.

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