Rosiglitazone

One of the core pathological features of type 2 diabetes mellitus is insulin resistance, and the advent of thiazolidinedione drugs provides a precise intervention pathway for improving this pathological state. As a representative variety of this class of drugs, rosiglitazone activates peroxisome proliferator-activated receptor γ (PPARγ) with high selectivity, regulates adipocyte differentiation, glucose transport and the expression of genes related to lipid metabolism, significantly enhances the sensitivity of peripheral tissues to insulin, and reduces circulating insulin levels. It is clinically mainly used for patients with type 2 diabetes mellitus whose blood glucose still fails to reach the target after diet control and exercise regulation. It can be used as a single drug, or in combination with metformin and sulfonylurea drugs, and is especially suitable for adult patients with obvious insulin resistance.

In recent years, the global market size of rosiglitazone preparations has remained at around USD 320 million. Affected by the iteration of similar hypoglycemic drugs and the early controversy over cardiovascular safety, the market growth has tended to be stable. Driven by the centralized procurement policy, the generic drug substitution rate in the Chinese market has exceeded 92%, and the terminal sales scale of public medical institutions in 2023 was approximately RMB 190 million. At present, the supply side of active pharmaceutical ingredients (APIs) has been dominated by domestic production. There are more than 15 domestic enterprises approved for production, the market competition is sufficient, and the price has dropped by more than 85% compared with that during the patent period. There is still a small amount of import demand only in the field of high-end customized APIs.

The original research enterprise of rosiglitazone is GlaxoSmithKline, and the original research trade name is "Avandia". The core compound patent expired in 2014 in the United States, and the Chinese compound patent expired in 2012. The main dosage forms approved by the original research are tablets, with specifications including 2mg, 4mg and 8mg. This product has been included in the *Catalogue of Reference Preparations for Chemical Drugs* of China, and is also a reference preparation announced by the FDA. Up to now, there are 27 rosiglitazone API registration numbers on the API Registration Platform of China Center for Drug Evaluation (CDE), among which 19 are in status A (activated, can be used for associated preparation declaration); the domestically approved rosiglitazone preparations on the market include three categories: tablets, dispersible tablets and capsules, involving 22 manufacturers. (Data as of June 2025, please refer to the official website of CDE for the latest information)

CATO can provide a full set of impurity reference standards for rosiglitazone API, covering all categories such as process impurities, degradation impurities and enantiomers. Most products have sufficient spot inventory. Spot orders placed before 16:00 can be shipped on the same day. All reference standards meet the requirements of multiple regulatory systems such as the Chinese Pharmacopoeia and FDA, and can meet the needs of the whole process of API R&D, registration declaration and quality control.