Cytisinicline Shows Promise as a Well-Tolerated and Effective Aid for Smoking Cessation
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Reviewed by Dat Tien Nguyen, B.A, ScM.
Translated by Nhi Phuong Quynh Le, B.A |
Posted on May 21st, 2025
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Smoking is one of the most prevalent risk factors contributing to millions of preventable deaths each year. While several smoking cessation aids such as bupropion and varenicline are currently available, their limited long-term effectiveness and notable side effect profiles highlight the need for new alternatives. Backed by funding from the biotechnology company Achieve Life Sciences, a clinical trial was conducted to evaluate the efficacy of cytisinicline in reducing nicotine cravings.
The phase 3 trial, conducted in the United States, enrolled 792 adult participants who reported smoking more than 10 cigarettes per day and expressed a desire to quit. Most participants had smoked for over 30 years and had attempted to quit an average of four times without success. Approximately 40% had previously used varenicline and 10% had tried bupropion. Nicotine gum and patches were also common in past cessation attempts.
Participants were randomly assigned to receive oral tablets three times daily containing either a placebo or 3 mg of cytisinicline. During the 12-week study, half of the cytisinicline group received active treatment for six weeks followed by six weeks of placebo to evaluate the durability of cessation effects. The other half continued cytisinicline treatment for the full 12 weeks. All participants received weekly behavioral support counseling. Cytisinicline is a plant-derived alkaloid that acts by binding to the α4β2 nicotinic acetylcholine receptors in the brain, competing with nicotine to help reduce cravings and alleviate withdrawal symptoms.
The results showed that cytisinicline significantly increased smoking cessation rates. After six weeks, approximately 15% of participants receiving cytisinicline had quit smoking, as confirmed by expired air carbon monoxide levels below 10 ppm—compared to only 6% in the placebo group. Among those who transitioned to placebo after six weeks, cessation rates remained stable at week 12, suggesting sustained effects. In contrast, participants who continued cytisinicline for the full 12 weeks saw cessation rates rise to 30%. In addition, cytisinicline was effective in reducing cravings, as measured by the Brief Questionnaire of Smoking Urges, and was generally well tolerated with minimal adverse effects.
The phase 3 trial, conducted in the United States, enrolled 792 adult participants who reported smoking more than 10 cigarettes per day and expressed a desire to quit. Most participants had smoked for over 30 years and had attempted to quit an average of four times without success. Approximately 40% had previously used varenicline and 10% had tried bupropion. Nicotine gum and patches were also common in past cessation attempts.
Participants were randomly assigned to receive oral tablets three times daily containing either a placebo or 3 mg of cytisinicline. During the 12-week study, half of the cytisinicline group received active treatment for six weeks followed by six weeks of placebo to evaluate the durability of cessation effects. The other half continued cytisinicline treatment for the full 12 weeks. All participants received weekly behavioral support counseling. Cytisinicline is a plant-derived alkaloid that acts by binding to the α4β2 nicotinic acetylcholine receptors in the brain, competing with nicotine to help reduce cravings and alleviate withdrawal symptoms.
The results showed that cytisinicline significantly increased smoking cessation rates. After six weeks, approximately 15% of participants receiving cytisinicline had quit smoking, as confirmed by expired air carbon monoxide levels below 10 ppm—compared to only 6% in the placebo group. Among those who transitioned to placebo after six weeks, cessation rates remained stable at week 12, suggesting sustained effects. In contrast, participants who continued cytisinicline for the full 12 weeks saw cessation rates rise to 30%. In addition, cytisinicline was effective in reducing cravings, as measured by the Brief Questionnaire of Smoking Urges, and was generally well tolerated with minimal adverse effects.