cyclosporine

Cyclosporine is a cyclic undecapeptide immunosuppressant derived from the fungus Tolypocladium inflatum. It acts as a calcineurin inhibitor and is primarily used to prevent organ rejection in kidney, liver, and heart transplants. Cyclosporine is also indicated for severe active rheumatoid arthritis (when other treatments fail), severe plaque psoriasis (unresponsive to other systemic therapies), nephrotic syndrome due to glomerular diseases (including steroid-dependent or resistant cases), Crohn's disease, eczema, and as ophthalmic drops for keratoconjunctivitis sicca (dry eyes). Its mechanism involves binding to cyclophilin in T cells to form a complex that inhibits calcineurin phosphatase activity. This blocks dephosphorylation of nuclear factor of activated T cells (NF-AT), reducing transcription of cytokines such as IL-2 required for T cell activation and proliferation[1][3][6]. Cyclosporine has significantly improved outcomes in transplantation medicine by specifically suppressing lymphocyte function.

Brand names

NeoralSandIMMUNEGengrafApo-cycloSPORINERestasis

Other names

环孢素ciclosporin