Ripretinib

In response to the clinical pain point of drug resistance in patients with advanced gastrointestinal stromal tumor (GIST) after multi-line treatment with tyrosine kinase inhibitors (TKI), ripretinib, as a novel switch control inhibitor, belongs to the class of broad-spectrum KIT/PDGFRA kinase inhibitor targeted drugs. Its mechanism of action breaks through the limitations of traditional TKIs. By dually binding to the kinase switch pocket and activation loop, it precisely inhibits various mutation types of KIT and PDGFRA, including the previously untreatable PDGFRA exon 18 D842V mutation. Currently, its approved indication is for patients with advanced GIST who have received 3 or more prior TKI therapies, filling the gap in the last-line treatment of GIST and bringing significant survival benefits to drug-resistant populations with no other treatment options.

The global market size of ripretinib had exceeded USD 210 million in 2022, with a compound annual growth rate of approximately 42% in the past three years. The growth momentum mainly comes from the continuous increase in the penetration rate of last-line treatment for advanced GIST and the advancement of clinical exploration for adjuvant treatment indications. In terms of the competitive landscape, only the original research product is on the market globally at present, and no generic drug has been approved in China. After being included in the National Medical Insurance Catalog in 2021, the payment threshold for patients has been greatly reduced, and the terminal volume expansion speed has accelerated significantly. The sales volume in domestic sample hospitals in 2023 increased by more than 110% year-on-year, and the generic drug market space will be considerable after the subsequent patent expiration.

Ripretinib was jointly developed by Zai Lab and Deciphera Pharmaceuticals as the original research enterprises, with the original trade name Qinlock®. Its core compound patent in China will expire in 2036. Currently, the original dosage form approved in China is tablet, with a specification of 50mg, which has been included in the China Listed Medicines Catalog as the reference listed drug. In terms of API registration, only the ripretinib API of the original research enterprise has completed the A-status registration with the Center for Drug Evaluation (CDE) at present. A number of domestic pharmaceutical enterprises have started the application work for generic drug research and development, and no domestic generic drug preparation has been approved for marketing yet. (Data as of November 2024, please refer to the official CDE website for the latest information.)

CATO can provide a full set of impurity reference standards for ripretinib API. Most products are available from stock, and stock orders placed before 16:00 can be shipped on the same day. All products meet the compliance requirements of multiple regulations such as the Chinese Pharmacopoeia and FDA, which can fully meet the reference standard needs of pharmaceutical enterprises in the whole process of generic drug research and development, quality research and production quality control.