Drug intelligence / Profile preview

varenicline

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intranasal
01

Overview

Varenicline is a small molecule medication primarily used as an aid for smoking cessation and also approved for the treatment of dry eye syndrome. It acts as a partial agonist at neuronal nicotinic acetylcholine receptors, with high selectivity for the alpha-4 beta-2 subtype. By partially stimulating these receptors and simultaneously blocking nicotine from binding, varenicline reduces cravings and withdrawal symptoms associated with quitting smoking. The drug was originally developed by Pfizer and first approved in 2006 under the brand name Chantix (now discontinued in some markets), but generic versions are widely available. Varenicline is considered one of the most effective pharmacological options for tobacco cessation[1][2][5][7].

Brand names
ChantixChampixTyrvaya
Other names
varenicline
02

Targets

α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)CHRNA7 (α7 nicotinic receptor)

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