The Smoking Cessation Aid Varenicline (Chantix, Champix): Drug Discovery Inspired by Natural Products

Abstract

Tobacco use remains the single largest preventable cause of morbidity in the United States, with approximately 440,000 premature deaths each year from smoking-related illnesses, such as cardiovascular disease, multiple types of cancer and pulmonary disease. The search for medications to assist people with their quit attempts has led to the introduction of three FDA approved first-line medications: 'safe' nicotine (Nicotine Replacement Therapy) in 1984, the antidepressant bupropion (Zyban) in 1997, and the α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist varenicline (Chantix, Champix) in 2006.