Tacrolimus is a potent immunosuppressive drug often administered to transplant recipient patients and exhibits a variety of adverse cardiovascular effects. Its mechanism of action involves the formation of a high affinity complex (Ki = 0.2 nM) with FK-506 binding protein 12 (FKBP12).

Cyclosporine A is an immunosuppressive agent, binds to the cyclophilin and then inhibits calcineurin with IC50 of 7 nM.