Trelagliptin

The long-term management of type 2 diabetes mellitus has extremely high requirements for medication compliance. Traditional DPP-4 inhibitors need to be taken daily, and patients have a relatively high risk of missed doses. As the world's first once-weekly DPP-4 inhibitor, trelagliptin inhibits the activity of dipeptidyl peptidase-4 with high selectivity, reduces the degradation of glucagon-like peptide-1, and continuously promotes insulin secretion to stabilize blood glucose levels. Its once-weekly dosing regimen greatly improves the convenience of medication for patients. It is mainly used clinically for blood glucose control in adults with type 2 diabetes mellitus. It can be used as monotherapy or in combination with other hypoglycemic agents, and is especially suitable for patient groups with irregular work and rest schedules who have difficulty adhering to daily medication.

The global trelagliptin market size exceeded USD 1.4 billion in 2023, with a compound annual growth rate of 8.2% in the past five years. The core growth driver comes from the increasing demand for long-acting hypoglycemic agents in chronic disease management. In terms of the Chinese market, as the prevalence of type 2 diabetes mellitus has risen to 11.9%, the penetration rate of long-acting hypoglycemic agents continues to grow. At present, more than 30 domestic enterprises have filed applications for generic drugs. After the implementation of centralized procurement, the price of winning bids has dropped by more than 70%, and the accessibility of drugs has been greatly improved. The expansion of the downstream preparation market directly drives the growth of demand for upstream API.

The original developer of trelagliptin is Takeda Pharmaceutical Company Limited of Japan, and the original brand name is Zafatek. Its core compound patent will expire in Japan in 2026. The core compound patent in China has been invalidated due to patent rejection. At present, only peripheral patents such as crystal form patents in China are still within the protection period. The main dosage form approved for the original product is tablet, with specifications of 50mg and 100mg. The 100mg specification has been included in the Catalogue of Marketed Drugs in China as the reference listed drug. As of now, there are more than 20 trelagliptin API registration records on China's CDE API registration platform, of which 12 have been activated and are eligible for associated review. 18 domestic enterprises have obtained marketing approval for trelagliptin generic preparations. (Data as of November 2024, please refer to the official CDE website for the latest information)

CATO provides a full set of impurity reference standards for trelagliptin API. Most products are available from stock. Stock orders paid before 16:00 can be shipped on the same day. All impurities meet the quality control requirements under multiple regulatory systems such as Chinese Pharmacopoeia and FDA. The research data such as impurity structure confirmation and purity calibration are complete, which can directly support the API quality research and generic drug consistency evaluation declaration work of pharmaceutical enterprises.