Varenicline tartrate -: Aid to smoking cessation -: Nicotinic α4β2 partial agonist

Nicotine addiction is one of the most prevalent addictive behaviors worldwide and more than half of the estimated 1.25 billion smokers will die from tobacco-related illness. Tobacco smoking induces and sustains a series of neurochemical events that are mediated via nicotine's agonist activity at neuronal nicotinic acetylcholine receptors (nAChRs). Current options for smoking cessation include nicotine replacement therapy, which can be effective but does not prevent nAChR activation, nicotine vaccines, which can block nicotine activation but may not improve craving and withdrawal, behavioral treatment and acupuncture, which are not always effective, and pharmacotherapy comprised of substances selectively targeting the action of nicotine. Researchers continue to investigate possible targets for the development of more effective agents to aid in smoking cessation. One promising agent to emerge is the partial a,P, nAChR agonist varenicline tartrate. This 3,5-bicyclic arylpiperidine selectively binds to the alpha(4)beta(2) nAChR and exhibits both potent preclinical partial agonist efficacy and safe and effective clinical activity. Varenicline has been submitted for regulatory approval in the U.S. and Europe for smoking cessation.