Imatinib

Chronic myeloid leukemia (CML) was once a hematological malignancy with an extremely poor prognosis, until the advent of tyrosine kinase inhibitors completely transformed the survival trajectory of patients. As the first small-molecule targeted anti-tumor drug approved worldwide, imatinib specifically blocks the kinase activity of the BCR-ABL fusion protein to inhibit abnormally proliferating leukemia cells. In addition to the treatment of all stages of Philadelphia chromosome-positive CML, it can also be used for the treatment of various malignant diseases such as KIT mutation-positive gastrointestinal stromal tumors and acute lymphoblastic leukemia, significantly increasing the 10-year survival rate of CML patients to over 80%, and is a milestone variety in the history of targeted drug R&D.

The global imatinib market size has remained stable for a long time, with a market size of approximately USD 4.2 billion in 2023, of which generic drugs account for more than 65%. In terms of the domestic market, the sales of imatinib at public medical institution terminals reached approximately RMB 1.8 billion in 2023. After being included in the centralized procurement in 2018, the winning bid price dropped by more than 90% compared with the peak price of the original research drug, greatly improving the accessibility of medication for patients. At present, 7 domestic enterprises have obtained approval for the marketing of generic imatinib. Under homogeneous competition, the stability of the API supply chain and the compliance of impurity research have become the core competitiveness of preparation enterprises.

The original research enterprise of imatinib is Novartis, with the brand name Gleevec®. The expiration date of its core compound patent in the United States is 2015, and the expiration date of the Chinese patent is 2013. The main dosage form approved for the original research product is tablet, with specifications including 100mg and 400mg, which has been included in the *Catalogue of Reference Preparations for Chemical Drugs* of China and the FDA Reference Preparation Catalogue. Regarding domestic API registration, as of now, there are 16 A-status registration numbers for imatinib mesylate (the commonly used salt form of imatinib API), covering multiple domestic and foreign manufacturers. A total of 11 domestic imatinib preparation products have been approved for marketing, covering tablets and capsules. (Data as of December 2024, please refer to the official CDE website for the latest information)

CATO provides a full set of impurity reference standards for imatinib API, covering all categories such as process impurities, degradation impurities, and enantiomers. Most products are in stock. For in-stock orders placed before 16:00, shipment can be arranged on the same day. All products meet the requirements of multiple regulatory systems such as the Chinese Pharmacopoeia and FDA, and can meet the needs of the whole process including API registration and declaration, process optimization, and quality research.