Varenicline

Smoking addiction is a chronic relapsing disease with a high global incidence. Long-term exposure to smoking can induce damage to multiple organs such as the respiratory system and cardiovascular system, and the drug options for clinical smoking cessation intervention have been limited for a long time. Varenicline is a highly selective partial agonist of the α4β2 nicotinic acetylcholine receptor. Its mechanism of action is that it can bind to this receptor to produce a moderate nicotine effect and alleviate withdrawal symptoms, and at the same time it can block the binding of nicotine to the receptor and reduce the reward feeling of smoking. It is a first-line drug recommended by current smoking cessation guidelines, and is mainly suitable for smoking cessation treatment of adult smokers, especially for people with previous withdrawal failures and severe withdrawal reactions.

The global smoking cessation drug market size was approximately USD 2.8 billion in 2023, and it is expected to grow at a compound annual growth rate of 6.2% to USD 3.8 billion by 2028. Among them, varenicline, with its clear efficacy advantages, accounts for approximately 37% of the smoking cessation prescription drug market share. In terms of the Chinese market, with the advancement of tobacco control policies and the improvement of public awareness of smoking cessation, the annual growth rate of varenicline prescriptions has exceeded 22% in the past three years. The current market is dominated by original research products, and 3 domestic enterprises have had their generic preparation products passed the consistency evaluation. After the implementation of centralized procurement, its accessibility is rapidly improving.

The original research enterprise of varenicline is Pfizer, with the trade name Chantix. Its core compound patent expired in the United States in 2020, and the Chinese compound patent expired in 2021. The main dosage form approved for the original research product is tablet, with specifications including 0.5mg and 1.0mg. It has been included in the *Catalogue of Reference Preparations of Chemical Drugs* of China, and is also a reference preparation recognized by the FDA. At present, there are 12 marketing registration information (status A) of varenicline API in China. In addition to the original research preparation, 4 domestic varenicline tablets have been approved for marketing. (Data as of June 2025, please refer to the official CDE website for the latest information)

CATO can provide a full set of impurity reference standards for varenicline API. Most products support spot supply, and spot orders placed before 16:00 can be dispatched on the same day. All products meet the requirements of multiple regulatory systems such as the Chinese Pharmacopoeia and FDA, and can fully meet the reference standard use needs of pharmaceutical enterprises in all stages of API R&D, quality research and registration declaration.