Tacrolimus (FK506) is a macrolide immunosuppressive drug that is approved for the prevention of allograft rejection. It is a standard component of immunosuppressive regimens currently in use for organ and reconstructive tissue transplants. The experimental literature has demonstrated potential efficacy in the management of other diseases for which transplantation does not play a role. The ability of tacrolimus to modulate the immune system and inhibit T cell activation provides a potential benefit for the treatment of disorders in which autoimmune phenomena are central to their pathogenesis such as rheumatoid arthritis and inflammatory bowel disease. Tacrolimus also has well-established neuroprotective and neuroregenerative properties through both similar and different mechanisms that have been extensively demonstrated in both small and large animal models. However, as a potent immunosuppressive agent, it can cause serious adverse effects, some of which are irreversible and potentially life threatening. This article reviews its safety under different therapeutic requirements and applications in both allogeneic and autogenous tissue reconstruction.
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