calcineurininhibitor
Calcineurin inhibitors are a class of immunosuppressive drugs that directly inhibit calcineurin, a calcium/calmodulin-dependent serine/threonine phosphatase essential for activating T-lymphocytes. By blocking calcineurin, these agents prevent dephosphorylation and nuclear translocation of the transcription factor NFAT, leading to reduced transcription of interleukin-2 and impaired T-cell proliferation.
The principal members of this class include cyclosporine and tacrolimus. Cyclosporine binds to cyclophilin, while tacrolimus
Clinical use centers on preventing organ transplant rejection and treating selected autoimmune diseases. Topical CNIs are
Pharmacokinetics and monitoring are characterized by substantial interindividual variability and a narrow therapeutic index. CNIs are
Adverse effects include nephrotoxicity, hypertension, neurotoxicity, tremor, hyperkalemia, and hyperglycemia. There is an increased risk of