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varenicline (Pfizer)
- Development stage
- Approved
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
**Varenicline** is a synthetic small-molecule smoking-cessation medicine originally developed by Pfizer. It is a high-affinity, selective partial agonist at neuronal nicotinic acetylcholine receptors containing alpha-4 and beta-2 subunits. Partial receptor stimulation helps reduce nicotine-withdrawal symptoms and craving, while competitive occupancy reduces nicotine-mediated reward signaling during tobacco use. The supplied SRI International study record concerns use of oral varenicline alongside telephone and web-based behavioral counseling; SRI International sponsored or participated in that behavioral-treatment study but did not originate varenicline. ([sri.com](https://www.sri.com/publication/education-learning-pubs/behavioral-counseling-and-varenicline-treatment-for-smoking-cessation/))
- Brand names
- ChampixChantixTyrvaya
- Other names
- vareniclinavarenicline tartratevareniclinum
02
Targets
α6β2 nAChR (α6β2 nicotinic receptor)α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)CHRNA7 (α7 nicotinic receptor)α3β2 nAChR (α3β2 nicotinic receptor)
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