On April 23, the varenicline tartrate tablets declared by Hausen Pharmaceuticals according to registration classification 4 have been approved by NMPA for marketing, which is the first imitation of the product in China.
Currently, commonly used first-line smoking cessation drugs include nicotine replacement therapy preparations, bupropion sustained-release preparations and varenicline.
Varenicline is a partial agonist of nicotine receptors.
Its structure is similar to nicotine.
It can bind to nicotine receptors, but the amount of dopamine released by nerve cells after binding is much less.
Varenicline was originally developed by Pfizer.
It was approved by the FDA in May 2006 and was approved to enter China in July 2008 under the trade name Changpei.
Pfizer Varenicline has global sales of US$919 million in 2020.
In 2009, the FDA added a black box warning to varenicline product instructions, emphasizing the risk of serious neuropsychiatric events of the drug, including behavioral changes, hostility, and depression.
A randomized, double-blind, placebo-controlled, and active-controlled large international multicenter clinical study published in the journal Lancet in 2016, code-named EAGLES, evaluated varenicline, bupropion, and nicotine patches Compared with placebo, the neuropsychological safety and smoking cessation efficacy of smokers with or without mental disorders.
The results of the study showed that varenicline does not increase the risk of negative neuropsychiatric events for smokers who have no history of mental disorders, and that varenicline is significantly more effective than nicotine transdermal patches and bupropion.
The withdrawal rate of Nicotiana treatment group was higher than that of placebo group (odds ratio [OR] 3.
61, 95% CI: 3.
24), nicotine patch group (1.
93) and bupropion group (1.
Based on the results of this study, the FDA removed the black box warning of varenicline related to serious neuropsychiatric side effects in December 2016, and China's National Food and Drug Administration also removed the black box warning in the product manual.
In addition to Hausen, Shandong Weizhi Encyclopedia Pharmaceutical has also applied for the listing of varenicline generic drugs and is currently undergoing NMPA review.