Apatinib

In response to the clinical pain point of limited options for later-line medication in the treatment of solid tumors such as advanced gastric cancer, the launch of apatinib, a small-molecule anti-angiogenic targeted drug, has filled the relevant treatment gap. As a small-molecule tyrosine kinase inhibitor independently developed in China, it can highly selectively bind to and inhibit the activity of vascular endothelial growth factor receptor 2 (VEGFR-2), block the transduction of downstream signaling pathways, and inhibit tumor angiogenesis, thereby exerting an anti-tumor effect. At present, apatinib monotherapy is approved for patients with advanced gastric adenocarcinoma or gastroesophageal junction adenocarcinoma who have progressed or relapsed after receiving at least 2 lines of systemic chemotherapy in the past. Meanwhile, it is also approved in combination with erlotinib for the first-line treatment of patients with locally advanced or metastatic non-small cell lung cancer with positive epidermal growth factor receptor (EGFR) gene mutations. Subsequent expansion of indications in fields such as liver cancer and thyroid cancer is also continuously advancing.

The market size of apatinib at the terminal of domestic public medical institutions has exceeded 3 billion yuan. With the continuous expansion of indications and the clinical popularization of combination medication regimens, the annual compound market growth rate has remained at around 12% in the past three years. At present, the market competition pattern is relatively concentrated, with original research products occupying a dominant position. Generic preparations from 3 enterprises have passed the consistency evaluation. In 2023, the oral regular-release dosage form of apatinib was included in the national centralized procurement catalog, and the price of the selected products decreased by more than 70%, which further reduced the medication burden of patients and also drove a steady increase in the demand for active pharmaceutical ingredients.

The original research enterprise of apatinib is Hengrui Medicine, with the trade name Aitan, and its core compound patent will expire in China in 2026. At present, the originally researched dosage form approved in China is tablets, with specifications including 0.25g, 0.375g and 0.425g, which have been included in the *Catalogue of Reference Preparations for Chemical Drugs* issued by the National Medical Products Administration. As of now, there are a total of 6 apatinib API registration entries on the API registration platform, among which 2 are A-status registration numbers that have been approved for use in marketed preparations. Apatinib tablets from 4 domestic enterprises, including Hengrui and 3 generic drug manufacturers, have been approved for marketing. (Data as of June 2025, please refer to the official CDE website for the latest information)

CATO provides a full set of impurity reference standards for apatinib API, most of which are in stock. Orders for in-stock products placed before 16:00 will be shipped on the same day. The products comply with the regulatory requirements of the Chinese Pharmacopoeia and FDA, and can fully meet the R&D and production needs of pharmaceutical enterprises in different scenarios such as impurity research, quality control and generic drug consistency evaluation.