Drug intelligence / Profile preview

cytisinicline

Development stage
Phase 4
Lead developer
Sonus Pharmaceuticals
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Cytisinicline is a naturally occurring plant-based alkaloid derived from the Fabaceae family, including Laburnum and Cytisus species. It is primarily used as a smoking cessation aid and acts as a partial agonist and partial antagonist at alpha-4 beta-2 nicotinic acetylcholine receptors in the brain. By weakly stimulating these receptors, cytisinicline reduces nicotine cravings and withdrawal symptoms while simultaneously blocking nicotine’s rewarding effects by preventing its binding to these receptors. Its mechanism of action is similar to varenicline but with lower receptor affinity, which may contribute to fewer side effects. Cytisinicline has been widely used in Eastern Europe under the brand name Tabex for decades and has recently undergone Phase 3 clinical trials in the US for smoking cessation. The drug is developed by Achieve Life Sciences.

Brand names
Tabex
Other names
baptitoxinesophorinecytisine
02

Targets

α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)CHRNA7 (α7 nicotinic receptor)

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