Comparison of radiolabeled bleomycins and gallium citrate in tumor-bearing mice

Abstract

Radioiodinated bleomycin is a chemically stable radiopharmaceutical that can be prepared with high specific activity using 123I. Its pharmacokinetics were compared with those of 99mTc,- 111In-, and 57Co-bleomycin, and 67Ga citrate in mice bearing a transplanted KHJJ tumor. The in vivo kinetics and stability of 123I- and 57Co-bleomycin were similar: both were acceptable, although not equivalent, tags for bleomycin and, along with 67Ga citrate, both had biologic properties suitable for tumor detection. Both 99mTc- and 111In-bleomycin dissociated rapidly in vivo and hence do not represent legitimate tags for bleomycin. However, 111In-bleomycin may have tumor-localizing properties related to its biochemical properties after the indium and chelate separate in vivo. Iodine-123 is superior to either 57Co or 55Co. Tumor-to-blood and tumor-to-liver ratios were higher for I-bleomycin than for 67Ga or Co-bleomycin. The nearly ideal nuclear properties of 123I should complement the biologic properties of bleomycin and lead to a useful tumor radiodiagnostic agent.