Tipiracil

In the clinical treatment of advanced colorectal cancer, fluorouracil drugs are core components of chemotherapy regimens, but traditional drugs have the shortcomings of low oral bioavailability and obvious toxic and side effects. As a thymidine phosphorylase inhibitor, tipiracil is a key component of the compound preparation TAS-102. Its mechanism of action is to inhibit the activity of thymidine phosphorylase, reduce the degradation of trifluridine in the same formulation, increase the exposure concentration of the latter in tumor tissues, and meanwhile reduce the gastrointestinal toxic and side effects caused by fluorouracil metabolites. At present, the compound preparation of tipiracil combined with trifluridine and trifluridine is mainly applicable to patients with metastatic colorectal cancer who have previously received fluorouracil, oxaliplatin and irinotecan-based chemotherapy, and who are not suitable for the above chemotherapy, and can also be used for the later-line treatment of some advanced gastric cancer.

Globally, the market size of tipiracil-related compound preparations had exceeded US$1.2 billion in 2023. Driven by the rising incidence of colorectal cancer and the increase in the penetration rate of later-line treatment, the compound annual growth rate remains at around 8%. In terms of the domestic market, following the approval and launch of relevant compound preparations in 2019, the sales volume in sample hospitals had exceeded RMB 700 million in 2023. The current market is still dominated by original research products, and 3 domestic pharmaceutical companies have submitted applications for the marketing of generic drugs. The implementation of centralized procurement in the future is expected to further improve clinical accessibility.

The original research enterprise of tipiracil is Japan's Taiho Pharmaceutical Co., Ltd., and the trade name of the original research compound preparation is Lonsurf. The core compound patent expires in 2020 in major markets such as Japan and the United States, and the compound patent in China expires in 2022. The main dosage form of the original research product on the market is tablet, with two specifications containing 7.065mg and 15.985mg of tipiracil per tablet, which has been included in the *Catalogue of Reference Preparations of Chemical Drugs* issued by the NMPA. Up to now, 4 domestic enterprises have had their tipiracil API reviewed by the CDE and obtained A-status registration numbers, and 1 enterprise has had its generic preparation 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 impurity reference standards for tipiracil, covering all categories such as synthetic process intermediates and degradation products. Most products are available from stock, and orders placed before 16:00 can be shipped on the same day. All products comply with the compliance requirements of multiple regulatory systems such as Chinese Pharmacopoeia and FDA, and can fully meet the reference standard needs of pharmaceutical enterprises in the stages of R&D, registration and quality control.