Tacrolimus NEW

Product Name: Tacrolimus
CAS: 104987-11-3
Appearance: White Powder
Purity: 99%
Certificates: ISO9001:2015; GMP

Overview
Tacrolimus is a macrolide antibiotic with potent immunosuppressive effects, widely used in preventing organ transplant rejection and treating autoimmune diseases. It works by inhibiting calcineurin phosphatase, suppressing T-cell activation and cytokine production. Compared to cyclosporine, tacrolimus offers stronger immunosuppressive effects with fewer side effects. In daily life, tacrolimus can also be used to treat moderate to severe atopic dermatitis in cases where the immune system is not compromised.

Mechanism of Action
Tacrolimus binds to FKBP-12 within T-cells, forming a complex that inhibits calcineurin activation. This suppression prevents interleukin-2 (IL-2) synthesis and T-cell infiltration into grafts, effectively reducing rejection risk. Its superior graft survival rates, better tolerance, and lower rejection incidence have made it a cornerstone in organ transplantation.

Clinical Importance and Market Overview
Tacrolimus is an essential anti-rejection drug for organ transplantation, with efficacy 10-100 times greater than cyclosporine. It also effectively treats immune diseases such as rheumatoid arthritis and lupus erythematosus. First launched by Japan's Astellas Pharma in 1993, tacrolimus formulations are now produced by four pharmaceutical companies in China. Global sales reached $2.655 billion in 2020, with domestic annual sales exceeding ¥6 billion. The price of the API can be as high as $50,000 per kilogram.

Research and Innovation

Supported by the National 863 Major Project, our research team utilized synthetic biology techniques to reconstruct high-yield production strains and precisely optimize fermentation processes. This resulted in high-performance and stable strains. Advanced separation and purification technologies were developed, effectively eliminating homolog impurities and reducing total API impurities to less than 1.0%, meeting USP-40 standards. The fermentation process has reached an internationally leading level, and the production cost of the API has been reduced to below 300,000 RMB/kg.

This project has been granted both Chinese and U.S. invention patents, ensuring comprehensive intellectual property rights. The product can be initially used for API production for export to international markets, followed by domestic new drug formulation registration.

Additionally, we are advancing the high-quality, high-yield optimization of production strains for two other critical immunosuppressive drugs used in organ transplantation: Sirolimus and Mycophenolate Mofetil, laying a solid foundation for future market applications.