Cytisinicline for Smoking Cessation in Adult Smokers

Abstract

Cytisinicline is a naturally derived, plant-based medication that has been developed as a treatment for smoking cessation and nicotine dependence. Based on a product available in Europe, over 4 million smokers in Central and Eastern Europe have used this medication and over 10,000 subjects have participated in clinical trials worldwide. Cytisinicline acts as a partial agonist and partial antagonist for the alpha-4 beta-2 nicotinic acetylcholine receptors in the brain, which are the same receptors that are activated by nicotine. Cytisinicline helps to reduce cravings, withdrawal symptoms and the reward and satisfaction associated with smoking by preventing nicotine from binding to these receptors and releasing dopamine. The On-going Research of Cytisinicline for Addiction-1 clinical trial has shown that participants receiving 3.0 mg cytisinicline three times daily had the highest biochemically verified point-prevalence abstinence rate (50%) compared with placebo (10%) at the end of treatment, with no significant safety concerns. These quit results were statistically significant (p<0.001). Cytisinicline demonstrates weak binding to the 5-hydroxytryptamine 3 receptor that causes nausea, consistent with few observed nausea events in participants receiving cytisinicline. No new medications for tobacco dependence have received United States Food and Drug Administration approval since 2006. Cytisinicline represents a promising treatment for those globally who continue to smoke tobacco.