tacrolimus + cyclosporine

Tacrolimus and cyclosporine are the two primary calcineurin inhibitors (CNIs) used as immunosuppressive agents in solid organ transplantation. Tacrolimus acts by binding to the immunophilin FKBP12, while cyclosporine binds to cyclophilin; both complexes subsequently inhibit the phosphatase activity of calcineurin. This inhibition prevents the dephosphorylation of the nuclear factor of activated T-cells (NFAT), thereby blocking the transcription of interleukin-2 (IL-2) and other pro-inflammatory cytokines essential for T-cell activation and proliferation. In the context of the ALTERNATION trial (NCT01551212) conducted by Hannover Medical School, these agents serve as the standard-of-care comparator group in liver transplant recipients. The trial investigates whether switching from a CNI-based regimen (either tacrolimus or cyclosporine) to an everolimus-based, CNI-free regimen can provide nephroprotection and reduce the long-term risk of chronic kidney disease associated with CNI therapy.

Brand names

Envarsus

Other names

tacrolimuscyclosporinecyclosporin A