Varenicline is a partial agonist at nicotinic acetylcholine receptors used as an aid in smoking cessation. Varenicline is a prescription medication used to treat smoking addiction.
- Mechanism
- Curator reviewed
Varenicline is an alpha-4 beta-2 neuronal nicotinic acetylcholine receptor partial agonist. The drug shows high selectivity for this receptor subclass, relative to other nicotinic receptors (>500-fold alpha-3 beta-4, >3500-fold alpha-7, >20,000-fold alpha-1 beta gamma delta) or non-nicotinic receptors and transporters (>2000-fold). The drug competitively inhibits the ability of nicotine to bind to and activate the alpha-4 beta-2 receptor. The drug exerts mild agonistic activity at this site, though at a level much lower than nicotine; it is presumed that this activation eases withdrawal symptoms.
- Primary indication
- For use as an aid in smoking cessation.Curator reviewed · 2 structured indications
- Formula / weight
- C13H13N3 · 211.268 g/mol (avg)
- First approval
- Canada, 2007 · United States, 2006 · European Union, 2016
- Code names
- CP-526,555
- Brand names
Resolves to
JQSHBVHOMNKWFT-UHFFFAOYSA-NSMILESC1C2CNCC1C1=C2C=C2N=CC=NC2=C1What you can answer from here — as of August 31, 2026
Which drugs share a target with Varenicline, and which of those have an active Phase 3 trial?
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