Sitagliptin

As a chronic metabolic disease affecting more than 500 million people worldwide, the emergence of dipeptidyl peptidase-4 (DPP-4) inhibitors provides a new path for oral hypoglycemic therapy that balances effectiveness and safety. Sitagliptin is a highly selective DPP-4 inhibitor. It reduces the degradation of glucagon-like peptide-1 (GLP-1) by inhibiting the activity of DPP-4, promotes insulin secretion and inhibits glucagon release in a glucose-dependent manner, so as to control blood glucose stably. This drug can be used as monotherapy for patients with type 2 diabetes mellitus who have poor blood glucose control after diet and exercise intervention, and can also be used in combination with metformin, insulin, etc. It is especially suitable for elderly patients or people prone to hypoglycemia. Long-term use does not increase the weight burden, and the incidence of adverse gastrointestinal reactions is low.

The peak global market size of sitagliptin once exceeded 4 billion US dollars. As patents expire one after another, the rapid entry of generic drugs has promoted the continuous adjustment of the market structure. In terms of the domestic market, the sales volume of sitagliptin-related dosage forms at public medical institution terminals exceeded 2.5 billion yuan in 2023, with a year-on-year growth of about 12%. At present, more than 30 enterprises have obtained approval for sitagliptin generic drugs. After winning the bid in the centralized drug procurement, the price of preparations has dropped by more than 90%, driving the continuous rise in the demand for upstream API. Local API enterprises are gradually occupying the dominant position in market supply by virtue of their cost advantages.

The original research enterprise of sitagliptin is Merck Sharp & Dohme, with the trade name Januvia. Its core compound patent expires in 2022 in the United States, and the Chinese compound patent expires in July 2022. The main dosage forms approved by the original research enterprise are tablets, with conventional specifications including 25mg, 50mg and 100mg. They have been included in the China Listed Drug Catalogue as reference preparations, and are also included in the FDA Reference Preparation Catalogue. Up to now, more than 40 domestic enterprises have completed the registration of sitagliptin APIs in CDE and obtained A status. In addition to single-agent tablets, sitagliptin and metformin compound preparations have also been approved for marketing. (Data as of October 2024, please refer to the official CDE website for the latest information)

CATO provides a full set of sitagliptin impurity reference standards, covering synthesis process impurities, degradation impurities and isotope labeled substances. Most of the products are in stock. Spot orders placed before 16:00 can be shipped on the same day. All products meet the compliance requirements of multiple regulations such as Chinese Pharmacopoeia, FDA and other regulations, and can fully meet the reference standard requirements for the whole process of API R&D, quality research and declaration.