Tacrolimus

Rejection after organ transplantation is the core risk affecting the long-term survival of patients. The advent of calcineurin inhibitors has brought a milestone breakthrough in the field of transplantation, and tacrolimus is the core representative of this class of drugs. It inhibits the activation and proliferation of T lymphocytes and reduces the release of inflammatory factors such as interleukin-2. Its immunosuppressive activity is 10-100 times that of cyclosporine. At present, it is the first-line drug for anti-rejection after solid organ transplantation such as liver, kidney, heart and lung transplantation, and is also widely used in the treatment of autoimmune diseases such as atopic dermatitis and systemic lupus erythematosus, covering multiple patient groups including adults and children.

The global market size of tacrolimus has exceeded USD 3 billion in 2023, with a compound annual growth rate of 4.2% in the past five years. Among them, the growth rate of the Chinese market is higher than the global average, with a compound annual growth rate of 6.8%, and the market size exceeded RMB 5.5 billion in 2023. In terms of competitive landscape, the original research product still accounts for about 35% of the high-end hospital market share. Domestic generic drugs have passed the consistency evaluation to achieve import substitution. At present, more than 20 enterprises have obtained preparation approvals, and the localization rate of APIs exceeds 70%. In the seventh batch of national centralized drug procurement, the average price reduction of tacrolimus oral regular-release dosage forms reached 63%, and the accessibility of drugs for patients has been greatly improved.

The original research enterprise of tacrolimus is Astellas Pharma, with the trade name Prograf. The core compound patents have expired in major markets such as Europe and the United States from 2008 to 2009, and the compound patent in China expired in 2007. At present, the dosage forms of the original research drug approved in China include oral capsules (0.5mg, 1mg, 5mg), injections (5mg/1ml) and topical ointments (0.03%, 0.1%), and multiple dosage forms have been included in the Chinese *Catalogue of Reference Preparations for Chemical Drugs* and the FDA Reference Preparation Catalogue. Up to now, the Center for Drug Evaluation (CDE) of the National Medical Products Administration of China has publicly announced more than 30 registration information of tacrolimus APIs, of which more than 20 are in status A (approved for use in marketed preparations), and nearly 30 tacrolimus preparation varieties have been approved for marketing in China. (Data as of October 2024, please refer to the official website of CDE for the latest information)

CATO can provide a full set of tacrolimus impurity reference standards, covering the full-dimensional research needs such as production process impurities and degradation impurities. Most of the products are in stock. Orders for in-stock products placed before 16:00 can be shipped on the same day. All reference standards comply with the compliance requirements of multiple regulatory systems such as the Chinese Pharmacopoeia and FDA, and can fully meet the use needs of various stages such as API research and development, quality research, and registration and declaration.