Azasetron

Chemotherapy-induced nausea and vomiting (CINV) is one of the most common adverse reactions in the treatment of tumor patients, with an incidence rate as high as over 70%. It not only reduces patients' treatment compliance, but may also lead to electrolyte disturbance and treatment interruption in severe cases. As a highly selective 5-hydroxytryptamine 3 (5-HT3) receptor antagonist, azasetron can block the 5-HT3 receptors in the central chemoreceptor trigger zone and peripheral vagus nerve endings to inhibit the signal transmission of the nausea and vomiting reflex, with an antiemetic effect lasting up to 24 hours. Compared with the first-generation同类 drugs, it has a lower incidence rate of adverse reactions such as extrapyramidal reactions and dizziness. It is clinically mainly used for the prevention and treatment of acute nausea and vomiting caused by tumor radiotherapy and chemotherapy and surgery, and the applicable population includes adult patients receiving moderately and highly emetogenic chemotherapy regimens, surgical patients requiring postoperative antiemetic intervention, etc.

In the domestic antiemetic drug market, 5-HT3 receptor antagonists have long accounted for nearly 60% of the market share. As a representative second-generation variety, azasetron had a domestic market size of approximately RMB 1.27 billion in 2023, with a compound annual growth rate of around 8.2% in the past three years. In terms of the competitive landscape, there are currently more than 20 domestic manufacturers of azasetron preparations that have been approved for marketing, among which injections are the core dosage form, accounting for more than 95% of the overall market share. Since 2021, multiple provinces have included azasetron in the scope of provincial centralized drug procurement, with an average price reduction of over 60% for the winning bids. The market share of the original research product has continued to shrink, domestic generic drugs have become the main force in the market, and the demand for localized API has also increased simultaneously.

The original research enterprise of azasetron is Japan's Yoshitomi Pharmaceutical Industries, Ltd., with the original brand name "Serotone". Its core compound patent in Japan expired in 2007, and the compound patent in China expired in 2008. The original research dosage form approved in China is mainly azasetron hydrochloride injection with the specification of 2ml:10mg, which has been included in the *Reference Listed Drug Catalogue of Chemical Drugs* issued by China's NMPA. As of now, there are a total of 13 azasetron API registration entries on the CDE API Registration Platform, among which 8 are in the status of "A" (approved for use in marketed preparations). More than 15 generic drugs of azasetron injection and oral dosage forms have been approved for marketing in China. (Data as of August 2024, please refer to the official CDE website for the latest information)

CATO can provide a full set of azasetron impurity reference standards. All products meet the compliance requirements of multiple regulations such as the Chinese Pharmacopoeia and FDA. Most products are in stock. Spot orders placed before 16:00 can be shipped on the same day, which can fully meet the various needs of pharmaceutical enterprises in the stages of impurity research, quality control and registration declaration.