Everolimus

Abnormal activation of the mTOR pathway is one of the core driving factors for tumor proliferation and immunosuppression. Everolimus, as a 40-O-hydroxyethyl derivative of sirolimus, belongs to the class of selective mTOR inhibitor anti-tumor and immunomodulatory drugs. It forms a complex with intracellular FK506 binding protein 12 to block the downstream signal transduction of mTOR kinase. On one hand, it can inhibit tumor cell cycle progression and angiogenesis, and is used for the treatment of solid tumors such as advanced renal cell carcinoma, pancreatic neuroendocrine tumor, and subependymal giant cell astrocytoma associated with tuberous sclerosis complex. On the other hand, it can inhibit the activation and proliferation of T cells and B cells, and is applied to prevent rejection after renal transplantation, covering the multiple clinical needs of patients with solid tumors, patients with rare diseases and organ transplant recipients.

The global everolimus market size was close to USD 2.8 billion in 2023. Although the entry of generic drugs after the expiration of core patents has pushed the overall market growth rate down to around 3%, the steady growth of demand in rare disease indications and transplantation immunology fields has become the core support of the market. In terms of the domestic market, the sales of everolimus in sample hospitals exceeded RMB 900 million in 2024, and the competition pattern is characterized by original research dominance and gradual penetration of generic drugs: currently, generic drug preparations from 4 domestic enterprises have passed the consistency evaluation, and in the 8th batch of nationally organized drug centralized procurement, the winning bid price of everolimus tablets dropped by more than 70%. With the expansion of medical insurance coverage, the domestic clinical accessibility is continuously improving.

The original research enterprise of everolimus is Novartis, with the trade name Afinitor®. Its core compound patent expired in 2018 in the United States and in 2019 in China. The main dosage forms approved by the original research include tablets and dispersible tablets, with specifications covering multiple doses such as 2.5mg, 5mg and 10mg. They have been included in the Catalogue of Listed Chemical Drugs in China and the FDA Reference Listed Drug Catalog, and are the legal reference standards for domestic generic drug research and development. In terms of API registration, more than 10 everolimus API registration numbers can be queried on the CDE platform at present, including the registration information of overseas manufactured APIs from Novartis, as well as a number of domestic APIs that have been approved for use in marketed preparations through the joint evaluation with preparations. Multiple everolimus generic preparations have been approved for marketing in China. (Data as of June 2025, please refer to the official CDE website for the latest information)

CATO can provide a full set of everolimus impurity reference standards, most of which are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. They fully comply with the compliance requirements of multiple regulations such as the Chinese Pharmacopoeia and FDA, and can provide stable reference standard support for API R&D, quality research and consistency evaluation work.