Capecitabine

The incidence of malignant gastrointestinal tumors such as colorectal cancer and gastric cancer continues to rise, and there is an urgent clinical demand for oral chemotherapy drugs with both efficacy and tolerability. Capecitabine is a fluorouracil prodrug, which can be converted into 5-fluorouracil by thymidine phosphorylase highly expressed in tumor tissues, and specifically acts on the S phase of the tumor cell cycle, inhibiting the DNA synthesis of tumor cells while reducing systemic toxic and side effects. As a single agent, it is indicated for adjuvant chemotherapy of colorectal cancer, and treatment of advanced metastatic gastric cancer and breast cancer. It can also be used in combination with other chemotherapeutic drugs for combination regimens for advanced solid tumors. Due to the advantage of convenient oral administration, it is especially suitable for out-of-hospital tumor patients requiring long-term maintenance therapy.

The global capecitabine market size has maintained steady growth in recent years, with the market size reaching approximately USD 1.38 billion in 2023, and the Chinese market accounting for nearly 35%. With the popularization of early screening for gastrointestinal tumors and the increase in the penetration rate of chemotherapy regimens, the compound annual growth rate is expected to remain around 3.2% in the next three years. After the expiration of the patent, the generic drug market has expanded rapidly. At present, more than 20 domestic enterprises have obtained approval for capecitabine generic drugs. Capecitabine has been included in the national centralized drug procurement for many times, and the price of winning bids has dropped by more than 80%, driving a substantial increase in clinical accessibility. The market share of the original drug has dropped to less than 15%.

The original developer of capecitabine is Roche, with the original brand name Xeloda. Its core compound patent in China expired in December 2013, and the formulation patent expired in 2021. The main dosage form approved for the original drug is tablet, with a conventional specification of 0.5g. It has been included in the *Catalogue of Reference Preparations for Chemical Drugs* of China, and is also listed in the FDA Reference Preparations Catalogue. At present, capecitabine API of more than 60 domestic enterprises has completed registration with the CDE, and the approved formulation varieties cover multiple dosage forms such as tablets and dry suspensions, which can fully meet clinical and generic drug development needs. (Data as of June 2025, please refer to the official CDE website for the latest information)

CATO can provide a complete set of impurity reference standards for capecitabine API, covering all categories such as process impurities and degradation impurities. Most products are available from stock. Stock orders placed before 16:00 can be shipped on the same day. All products meet the requirements of multiple sets of regulations such as the Chinese Pharmacopoeia and FDA, and can provide stable compliance support for generic drug quality research, consistency evaluation, and quality control in the production process of APIs.