What Is Tacrolimus?

Tacrolimus, also known as FK506, is a fermentation product isolated from streptomyces tsukubaensis. Its chemical structure is a 23-membered macrolide antibiotic. It is a powerful new type of immunosuppressive agent. It mainly suppresses the release of interleukin-2 (IL-2), and comprehensively suppresses T lymphocytes, which is 100 times stronger than cyclosporine (CsA). In recent years, it has been marketed in 14 countries including Japan and the United States as a first-line drug for liver and kidney transplantation. Clinical experiments have shown that it has a good effect in heart, lung, intestine, bone marrow transplantation. At the same time, FK506 also plays an active role in the treatment of autoimmune diseases such as atopic dermatitis (AD), systemic lupus erythematosus (SLE), and autoimmune eye diseases.

Tacrolimus

Tacrolimus, also known as FK506, is from

[3S- [3R [E (1S, 3S, 4S)], 4S, 5R, 8S, 9E, 12R, 14R, 15S, 16R,

18S, 19S, 26aR)]-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecane-5, 19-dihydroxy -3- [2- (4-hydroxy-3-methoxycyclohexyl) -1-methylvinyl] -14, 16-dimethoxy-4,10,12,18-tetramethyl- 8- (2-propenyl) -15,19-epoxy-3H-pyrido [2,1-c] [1,4] oxazaazatricosane-1,7,20,21 (4H, 23H) -tetraketone monohydrate

At the molecular level, the role of tacrolimus is clearly to combine with cellular proteins (FKBP12), and accumulate in cells to produce utility. The FKBP12-tacrolimus complex specifically binds and inhibits calcinurin, which inhibits the action of calcium-dependent signaling pathways produced in T cells, thus preventing the transcription of discontinuous lymphokine genes. This drug is a highly immunosuppressive drug, and its activity has been confirmed in vitro and in vivo experiments. This drug inhibits the formation of cytotoxic lymphocytes that form major transplant rejection. This medicine inhibits T cell activation and T helper cell dependent B cell proliferation. It also inhibits the production of lymphokines such as interleukin-2, interleukin-3, and gamma-interferon and the expression of interleukin-2 receptors. At the molecular level, the effect of this drug appears to be caused by binding to a cellular protein (FKBP), which also causes the compound to accumulate in cells. The drug was found to be effective in liver and kidney transplantation in in vivo tests.

Liver, heart, kidney and bone marrow transplant patients are the first choice for immunosuppressive drugs. Post-transplant rejection is resistant to traditional immunosuppressive regimens. This drug can also be used. Adverse reactions were similar to cyclosporine.

The following oral and

Due to the severe illness of most users and the concomitant use of many other drugs, it is often difficult to determine the adverse reactions associated with immunosuppressive drugs. There is evidence that many of the following

Capsules 1mg * 10 capsules, 50 capsules, 5mg * 5 capsules, 50 capsules. Injection 5mg / 1ml * 10 ampoules.