tacrolimus

Tacrolimus is a macrolide immunosuppressant primarily used to prevent organ rejection in patients who have received kidney, liver, heart, or lung transplants. It is also used topically for moderate to severe atopic dermatitis and other inflammatory skin conditions. Tacrolimus acts by binding to the immunophilin FKBP-12 (FK506 binding protein), forming a complex that inhibits the phosphatase activity of calcineurin. This inhibition blocks T-lymphocyte signal transduction and interleukin-2 (IL-2) transcription, thereby suppressing immune responses that would otherwise lead to transplant rejection or inflammation. Tacrolimus was discovered from Streptomyces tsukubaensis in 1984 and has similar activity to cyclosporine but with lower rates of acute rejection. It was developed by Fujisawa Pharmaceutical (now part of Astellas Pharma).

Brand names

PrografAstagraf XLEnvarsus XRHecoria

Other names

tacrolimus