Varenicline is the first pharmacological aid for smoking cessation treatment to be approved in almost a decade. Varenicline is an α4β2 nicotinic acetylcholine receptor partial agonist. It may assist those who wish to quit smoking by producing partial activation at nicotinic receptors to ease craving and withdrawal symptoms; and by simultaneously blocking the effects of nicotine from cigarettes smoked, thereby reducing the satisfaction of continued smoking. The effectiveness of varenicline as an aid for smoking cessation has been demonstrated in several clinical trials versus placebo and sustained release bupropion. In addition, varenicline is well tolerated and has an acceptable safety profile. As an aid for smoking cessation, varenicline offers progress in the treatment of tobacco dependence.