As a reflection of an exponential increase in smoking rates throughout the world during the last century, the economic and human burden of mortality and morbidity related to smoking is now clearly defined. Smoking cessation is associated with health benefits for people of all ages. In this paper we provide a comprehensive review of current licensed pharmacological smoking cessation agents including efficacy and safety profiles, with comparisons of individual therapies available. Furthermore, we offer a prospective on the need for further testing of other agents including novel avenues of therapy.