Cytisinicline is a plant-based alkaloid with a high binding affinity to the nicotinic acetylcholine receptor. It is an established smoking cessation treatment that has been approved and marketed in Central and Eastern Europe for more than 20 years.
Mechanism of Action (MOA)
Cytisinicline’s dual-acting MOA specifically targets the α4β2 nicotine receptor. Through its partial agonist/partial antagonist activity, it is believed to help reduce nicotine cravings, withdrawal symptoms and reward and satisfaction associated with smoking.
The α4β2 nicotinic receptor is a well-understood target in addiction. When nicotine binds to this receptor, it causes dopamine to be released reinforcing the dopamine reward system. This receptor has been implicated in the development and maintenance of nicotine dependence. Cytisinicline is believed to act as a partial agonist, preventing nicotine from binding and releasing dopamine.
Cytisinicline process – Click image to view full-size.