Drug intelligence / Profile preview

varenicline oxalate + varenicline tartrate

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of two salt forms of the same active pharmaceutical ingredient, varenicline—specifically, varenicline oxalate and varenicline tartrate. Varenicline is a partial agonist at the α4β2 subtype of neuronal nicotinic acetylcholine receptors. It works by partially stimulating these receptors while simultaneously blocking nicotine from binding, thereby reducing cravings and withdrawal symptoms associated with smoking cessation. Both salt forms have been shown to be pharmacokinetically equivalent in delivering active varenicline to the body and are generally well tolerated[1][3]. Varenicline is primarily indicated as an aid for smoking cessation therapy[2][5][7].

02

Targets

α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)HTR3A (5-hydroxytryptamine receptor 3A)Muscle-type nicotinic acetylcholine receptorCHRNA7 (α7 nicotinic receptor)

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