New fluorescent derivatives of cyclosporin for use in immunoassays

The synthesis of new fluorescent derivatives of cyclosporin is described and their affinity with the specific Sandoz monoclonal antibody investigated. Synthesis was carried out using cyclosporin-C-hemisuccinate as the starting material with monodansylcadaverine, 4-bromomethyl-7-methoxycoumarin, and 4-bromomethyl-6,7-dimethoxycoumarin as labels. After extraction the derivatives were purified by HPLC and their binding affinity with the monoclonal antibody evaluated by the Incstar Cyclo-Trac SP radioimmunoassay. All three derivatives showed good binding and it is suggested that they may be of use in an immunoassay for measuring cyclosporin.