Use of 125I-labeled-histamine-cyclosporin C for monitoring serum cyclosporine concentrations in transplantation patients.

We synthesized an 125I-labeled-histamine-cyclosporin C tracer, to obviate the use of tritiated tracer in radioimmunoassay of cyclosporine. With this tracer, the assay results varied linearly with concentration up to at least 800 micrograms/L. The within-assay CV was 6.6% at 39 micrograms/L, 4.2% at 100 micrograms/L, and 7.0% at 300 micrograms/L (n = 15). The between-assay CV was 10.0, 6.4, and 7.8% for the same respective concentrations. Comparison with an assay involving tritiated tracer (x) showed good agreement of results: y = 3.81 + 0.927x (r = 0.975, n = 604). Analytical recovery ranged from 100 to 106%. We also compared another commercially available radioiodinated tracer ("125Iodocyclosporin"; Immunonuclear Corp.). Our tracer appeared to be more specific for cyclosporine, as determined by assaying chromatographic fractions of bile extract from a patient being treated with cyclosporine. Results with use of our tracer compared favorably with those obtained with the tritiated tracer, and our assay has the advantages of gamma counting vs liquid-scintillation counting.