Tacrolimus

Tacrolimus, also known as FK506, a fermentation product isolated from Streptomyces, is a macrolide antibiotic and a powerful new immunosuppressant, which mainly inhibits the release of interleukin-2 (IL-2) and comprehensively inhibits the action of T lymphocytes, which is 100 times stronger than cyclosporin (CsA). In recent years, as a first-line drug for liver and kidney transplantation, it has been marketed in 14 countries such as Japan and the United States. Clinical experiments have shown that it has good efficacy in heart, lung, intestine, bone marrow transplantation. At the same time, FK506 also plays a positive role in the treatment of atopic dermatitis (AD), systemic lupus erythematosus (SLE), autoimmune eye disease and other autoimmune diseases.

Melting point: 113-115℃
Boiling point: 871.7℃
Flash point: 481.0℃
Density: 1.19g/cm3
Appearance: White or off-white crystalline powder
Refractive index: 1.549

At the molecular level, tacrolimus apparently acts by binding to a cellular protein (FKBP12), which accumulates in the cell to produce its effect. The FKBP12-Tacrolimus complex specifically binds to and inhibits calcineulin, which inhibits calcium-dependent message pathways produced in T cells, thereby preventing the transcription of discontinuous lymphokine genes. This drug is highly immunosuppressive, and its activity has been confirmed in vitro and in vivo. The drug inhibits the production of cytotoxic lymphocytes that are responsible for major graft rejection. It inhibits the activation of T cells and the proliferation of T helper cells dependent on B cells. It also inhibits the production of lymphatic factors such as interleukin-2, interleukin-3, and gamma-interferon, and the expression of interleukin-2 receptors. At the molecular level, the effect of the drug appears to be caused by binding to a cellular protein (FKBP), which also causes the compound to accumulate between cells. In vivo, the drug has been shown to be effective in liver and kidney transplantation.

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