Iodinated Bleomycin: An Unsatisfactory Radiopharmaceutical for Tumor Localization.
Abstract
Cobalt-57 bleomycin is a clinically useful tumor localizing agent, but attempts to label bleomycin (BLEO) with other radionuclides have been made because of the long physical half-life of Co(57). As an alternative labeling approach, BLEO was iodinated both directly on the imidazole ring and indirectly by reaction with N-succinimidyl 3-(4-hydroxy, 3-iodophenyl) propionate. Directly iodinated BLEO retained antibacterial activity, but in tumor-bearing rats showed a lower tumor to blood ratio at 2 hours (2.3) than was obtained with Co(57) BLEO (11.8). The antibacterial activity of the indirectly labeled BLEO was markedly reduced and this material showed a tumor to blood ratio at 2 hours of 0.55.
Document Details
- Document Type
- Technical Report
- Publication Date
- Mar 01, 1976
- Accession Number
- ADA024095
Entities
People
- B. A. Siegel
- H. Kubota
- T. Komai
- W. C. Eckelman
- W. J. Rzeszotarski
Organizations
- Armed Forces Radiobiology Research Institute