Pharmacology of CsA and FK-506

Summary

Cyclosporine A and FK-506 are two distinct chemical entities which share a common mechanism of action and induce a quite unique selective immunosuppression. Once complexed with two different classes of abundant intracellular proteins called immunophilins, they acquire the property to block the enzymatic activity of calcineurin. In activated T helper cells, this prevents the activation of several lymphokine genes with dramatic consequences for the development and maintenance of cellular and humoral response. The effectiveness of these drugs in organ transplantation and autoimmune diseases has been widely verified, both in animal models and clinically.

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Di Padova, F.E. Pharmacology of CsA and FK-506. Perspectives in Drug Discovery and Design 2, 49–56 (1994). https://doi.org/10.1007/BF02171736

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Key words

  • Cyclosporine A
  • FK-506
  • Immunosuppressive drugs
  • Immunosuppression