Linagliptin

As a chronic metabolic disease with high incidence worldwide, diabetes mellitus has seen DPP-4 inhibitors become one of the core second-line hypoglycemic options due to their clinical advantages of stable hypoglycemic effect, low risk of hypoglycemia, and no impact on body weight. Linagliptin is a representative variety of highly selective, long-acting DPP-4 inhibitors. By reversibly inhibiting the activity of dipeptidyl peptidase-4, it prolongs the action time of endogenous GLP-1 and GIP, thereby promoting insulin secretion and inhibiting glucagon release in a glucose-dependent manner. It is clinically mainly used to improve glycemic control in patients with type 2 diabetes mellitus, and can be used as monotherapy or in combination with metformin and sulfonylureas. It is especially suitable for elderly patients with combined renal insufficiency, and no dosage adjustment is required.

The global market size of linagliptin exceeded USD 3.5 billion at its peak in 2020. With the expiration of core patents and the gradual entry of generic drugs, the market size has declined in recent years, but still maintains an annual sales volume of more than USD 1.5 billion, among which the Chinese market share has increased year by year to about 12%. At present, the competition of generic drugs in China is of moderate intensity. Linagliptin generic drugs from more than 15 enterprises have been approved for marketing, and have been included in the national centralized procurement catalog. The price of the winning products has dropped by more than 90% compared with the original research drug. The expansion of downstream preparation production capacity has driven the continuous rise of demand for APIs. In 2023, the domestic consumption of linagliptin API increased by 41% year-on-year.

The original research enterprise of linagliptin is Boehringer Ingelheim, with the original trade name Trajenta, and its core compound patent expired in China in 2023. The main dosage form approved for the original research drug is tablet, with a specification of 5mg. 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, linagliptin APIs from more than 20 domestic enterprises have completed registration with the CDE and obtained Class A status, which can be associated with preparation declaration or marketed. Except for the original research drug, all linagliptin preparations approved in China are generic drugs, covering multiple dosage forms such as tablets and metformin compound preparations. (Data as of October 2024, please refer to the official CDE website for the latest information)

CATO provides a full set of impurity reference standards for linagliptin API, covering all categories such as synthesis process impurities, degradation impurities and enantiomers. Most products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. All reference standards meet the compliance requirements of multiple regulations such as the Chinese Pharmacopoeia and FDA, and can meet the reference substance needs of the whole process of API R&D, quality research and declaration.