Tacrolimus

1、Nomenclature
English name：Tacrolimus

2、Structural formula

Molecular formula：C₄₄H₆₉NO₁₂S    
Molecular mass：804.02    
CAS No.：104987-11-3

   
3、Mechanism and clinical use:

Tacrolimus is strong-efficacy macrolide immunosuppressant. At the molecular level, its effect is mediated through protein FKBP12 in cytoplasm which is binding with it.FKBP12 makes Tacrolimus into cell and form a complex that competitively binds specifically to calmodulin and inhibits calmodulin (the latter mediates calcium-dependent inhibitory signal transduction system in T-cells), so as to block a series Gene transcription of lymphokine. In-vitro experiments demonstrate that Tacrolimus is strong-efficacy immunosuppressant, it can inhibit formation of cytotoxic lymphocytes, and allograft rejection is mainly caused by the latter.

This drug inhibits activation of T-cells,TH-cell-dependent B-cells-propagation,and generation of lymphokine such as express of interleukin 2, interleukin 3, β-interferon and interleukin 2 receptor. Tacrolimus can inhibit allograft rejection of skin, heart, kidney and liver, extend survival time of allograft, and this is evidenced in bodies of rodent, dogs, primate and human. It has been widely used for acute and chronic rejection of liver, kidney and bone marrow transplantation.

4、Executive standards
CP、EP、USP

5、Qualification certificate
Registration of "A" status, Chinese GMP; WC license, COPP certificate, CEP certificate, US DMF registration number; MFDS Registration Certificate

6、Packaging size specification

Inner package: single-layers polyethylene bag and aluminum foil bag.

Outer package: Medicinal aluminum bottle.

Packaging size: 500 g/bottle