Montelukast

Asthma and allergic rhinitis, as highly prevalent chronic respiratory diseases, have long plagued more than 500 million patients worldwide. The adverse reactions of traditional hormone drugs limit their long-term use, and the emergence of leukotriene receptor antagonists provides a safer option for clinical practice. Montelukast is a highly selective cysteinyl leukotriene receptor antagonist. By blocking the binding of leukotriene in the airway to its receptor, it inhibits airway constriction, mucus secretion and increased vascular permeability caused by the release of inflammatory mediators, and achieves anti-inflammatory and anti-asthmatic effects without the involvement of hormones. It is mainly clinically used for the prevention and long-term treatment of asthma in people aged 2 years and above, and can also relieve symptoms of seasonal and perennial allergic rhinitis. Due to its convenient administration and good tolerance, it is a first-line commonly used drug for the treatment of respiratory diseases in children.

At present, the global market size of montelukast is stable at around USD 2.5 billion, the annual sales volume in the Chinese market is approximately RMB 4.5 billion, and the compound annual growth rate is maintained at a stable level of 5%. After the patent of the original research product expired, generic drugs have been launched rapidly. More than 80 domestic enterprises have obtained the approval documents for montelukast preparations, and more than 30 enterprises produce APIs. Since 2020, multiple rounds of national centralized procurement have reduced the prices of montelukast sodium tablets, granules and other dosage forms by an average of 70%. The market share of generic drugs in public medical institutions has exceeded 90%, and the demand for upstream APIs continues to be released along with the increase in the penetration rate of primary medical medication.

The original research enterprise of montelukast is Merck Sharp & Dohme, and the original trade name is "Singulair". Its core compound patent expired in the United States in 2012, and the core patent in China also expired in 2012. The main dosage forms approved for the original research include 4mg and 5mg chewable tablets, 4mg granules and 10mg film-coated tablets, which have been included in the *Catalogue of Chemical Reference Preparations* of China and the FDA reference preparation catalogue. In terms of domestic API registration, as of now, there are more than 30 registration numbers of montelukast sodium APIs, most of which are in status A and can be used for associated review. Multiple dosage forms of generic montelukast have been approved for marketing in China. (Data as of August 2025, please refer to the official website of CDE for the latest information)

In response to the impurity control needs in the R&D and production process of montelukast, CATO can provide a full set of impurity reference standards for this API, covering the whole chain of impurity types including synthetic starting materials, intermediates, degradation products, etc. Most of the products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. All reference standards comply with the compliance requirements of multiple regulations such as the Chinese Pharmacopoeia and FDA, and can fully support the methodological validation, quality research and registration declaration work of pharmaceutical enterprises.