This study provides pharmacologic evidence that cytisinicline selectively interacts with the α4β2 nicotinic receptor while exhibiting minimal interaction with the 5-HT3 receptor, a key mechanism potentially underlying its improved gastrointestinal tolerability. These findings help explain the lower nausea rates observed in clinical trials and support cytisinicline as a promising alternative to varenicline for smoking cessation, particularly in individuals sensitive to medication-related side effects. This receptor-specific profile may enhance treatment adherence and expand the appeal of pharmacologic smoking cessation strategies.
Rubinstein et al. (Thu,) studied this question.