Class/mechanism: Immunosuppresive medication, calcineurin-inhibitor, inhibits T-cell activity. Exact mechanism of action unknown, but it may involve tacrolimus binding to the intracellular protein FKBP-12, which results in the formation of a complex of tacrolimus, FKBP-12, calcium, calmodulin, and calcineurin. This complex inhibits calcineurin's phosphatase activity and may prevent NF-AT (nuclear factor of activated T-cells) activity, which is believed to be responsible for transcription of lymphokines such as interleukin-2 and gamma interferon). Tacrolimus's activity may involve inhibiting humoral immunity and cell-mediated reactions such as graft versus host disease, allograft rejection, collagen-induced arthritis, delayed type hypersensitivity, and experimental allergic encephalomyelitis.
Route: PO, IV
Extravasation: no information
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Patient drug information
Also known as
- Code name: FK-506
- Brand names: Advagraf, Prograf