Products
Priluxid®
Pharmacotherapeutic group
Immunosuppressant, calcineurin inhibitorInternational name
TacrolimusDosage form
CapsulesProduct information
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Immunosuppressant. At the molecular level, effects and intracellular levels tacrolimus appear to be mediated by binding to a cytosolic protein (FKBP12). The FKBP12- tacrolimus complex specifically and competitively binds to and inhibits calcineurin, leading to a calcium-dependent inhibition of T-cell signal transduction pathways, thereby preventing transcription of a discrete set of cytokine genes.
Tacrolimus is a highly potent immunosuppressive agent. In the vitro and in vivo experiments, tacrolimus inhibited the formation of cytotoxic lymphocytes, which are mainly responsible for graft rejection. Tacrolimus suppresses the formation of lymphokines (such as interleukins-2, -3, and γ-interferon) and the expression of the interleukin-2 receptor, and T-helper-cell dependent B-cell proliferation.