cyclosporine + tacrolimus

Cyclosporine + tacrolimus is a combination of two immunosuppressant drugs, both classified as calcineurin inhibitors. These agents are primarily used to prevent organ rejection in transplant recipients and to treat certain severe autoimmune diseases. Cyclosporine is a cyclic endecapeptide, while tacrolimus is a macrocyclic lactone; despite their structural differences, both drugs inhibit the phosphatase activity of calcineurin by forming complexes with intracellular proteins (cyclophilin for cyclosporine and FKBP12 for tacrolimus). This inhibition prevents dephosphorylation and nuclear translocation of the nuclear factor of activated T-cells (NFAT), suppressing transcription of interleukin 2 and other cytokines critical for T-cell activation. Both drugs are associated with similar adverse effects such as nephrotoxicity, neurotoxicity, hypertension, hyperglycemia, infections, and increased risk of malignancy[1][5][8]. Tacrolimus tends to be more potent than cyclosporine at lower concentrations[1]. The combination may be considered in select clinical scenarios but is not standard due to overlapping toxicities.

Other names

FK506 (for tacrolimus)CsA (for cyclosporine)