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
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.
Patient drug information
- Tacrolimus (Prograf) package insert PDF pages 38-42
- Tacrolimus (Prograf) patient drug information (UpToDate)
Also known as
- Code name: FK-506
- Brand names: Advagraf, Prograf, Tacforius