Gimeracil

In the clinical treatment of advanced pancreatic cancer, colorectal cancer and other malignant gastrointestinal tumors, the chemosensitivity of fluoropyrimidine drugs has always been the core breakthrough to improve the efficacy. Gimeracil, as one of the core components of compound oral fluoropyrimidine preparations, belongs to dihydropyrimidine dehydrogenase (DPD) inhibitors. Its mechanism of action is to irreversibly inhibit the degradation of fluorouracil by DPD, prolong the effective action time of fluorouracil in vivo, reduce the dosage of administration and reduce toxic and side effects at the same time. At present, gimeracil is mainly formulated into compound preparations together with tegafur and oteracil potassium, which are used for first-line and palliative chemotherapy for unresectable advanced/metastatic gastric cancer, colorectal cancer and pancreatic cancer. It is an important part of oral chemotherapy regimens for gastrointestinal tumors, and is suitable for elderly patients and people who cannot tolerate intravenous chemotherapy.

The global market size of compound preparations containing gimeracil has exceeded USD 2.8 billion in 2023, with a compound annual growth rate of 6.2% in the past five years. Among them, the proportion of the Chinese market has increased from 12% in 2019 to 21% in 2023, and the growth drivers mainly come from the rising incidence of gastrointestinal tumors and the advantage of medication compliance of oral chemotherapy. In terms of the competitive landscape, the original research product still accounts for about 45% of the market share, and 3 domestic enterprises have been approved to manufacture the generic compound preparation. After the compound preparation was included in the national centralized procurement in 2022, the price dropped by 68%, and the demand of downstream preparation enterprises for cost-effective gimeracil API has been released rapidly.

The original research enterprise of gimeracil is Taiho Pharmaceutical Co., Ltd. of Japan, and the trade name of its original research compound preparation is "爱斯万 (S-1)". The core compound patent of gimeracil expired in 2021 in major markets such as Japan and the United States, and the compound patent in China expired in 2020. The main dosage form approved by the original research is compound tablet, each containing 25 mg of gimeracil. This original research compound preparation has been included in the *Catalogue of Reference Preparations of Chemical Drugs* of China, and is also included in the FDA Reference Preparations Catalogue. Up to now, 7 enterprises have submitted registration numbers for gimeracil API on the API registration platform of China CDE, among which 4 have been publicized with A status, and 11 domestic enterprises have been granted the marketing authorization for this compound preparation. (Data as of September 2024, please refer to the official website of CDE for the latest information)

CATO can provide a full set of impurity reference standards for gimeracil API, covering a total of 12 process impurities and degradation impurities. Most of the products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. All reference standards meet the requirements of multiple regulatory systems such as Chinese Pharmacopoeia and FDA, and can fully support the full-process requirements of API registration, preparation declaration and quality research.