Pharmacokinetics of bleomycin in man - III. Bleomycin 57Co Vs Bleomycin

D. S. Alberts, Hsiao Sheng G. Chen, J. M. Woolfenden, T. E. Moon, Sai Y. Chang, J. N. Hall, K. J. Himmelstein, J. Gross, S. E. Salmon

Research output: Contribution to journalArticlepeer-review

10 Scopus citations

Abstract

Of all the bleomycin-containing radiopharmaceuticals, bleomycin 57Co has proven the most useful whole-body tumor-imaging agent. We have studied its in vitro physicochemical properties and in vivo disposition in animals and man to optimize its use as a scanning agent. High-pressure liquid chromatographic analysis of the standard bleomycin 57Co preparation (1 unit bleomycin plus 1 mCi chloride 57Co showed it to contain 1% free chloride 57Co). Dialysis experiments showed that bleomycin 57Co does not dissociate as it diffuses through a dialysis membrane. In nine patients, bleomycin 57Co had a t12/βof 3.4 h, a t12/γof 45.8 h, a Vd of 12.1 liters/m2 and a 24-h urinary excretion of 82.1% of the administered dose. In comparison, bleomycin, assayed by radioimmunoassay, had a terminal phase plasma t1/2 of only 4.0 h, a similar Vd (17.3 liters/m2), and a 24-h urinary excretion of only 44.8%. Bleomycin 57Co tumorto-plasma concentration ratios ranged from 14.1-23.8 at 1 day to 5.4 at 2 days after administration. Our finding that tumor imaging with bleomycin 57Co is best achieved at 24 h is well explained by its almost complete urinary elimination in the first few hours after administration and the peak tumor-to-plasma ratio achieved at 24 h. One disadvantage of bleomycin 57Co as a scanning agent is its very extended plasma t1/2 In rabbits chloride 57Co has the same prolonged plasma terminal elimination phase (t12/γ) as our standard bleomycin 57Co preparation, which contains chloride 57Co as a 1% impurity. Removal of this impurity prior to scanning or use of cold cobalt chloride to help eliminate it from the plasma might result in a shortened bleomycin 57Co plasma t12/γ.

Original languageEnglish (US)
Pages (from-to)33-40
Number of pages8
JournalCancer Chemotherapy And Pharmacology
Volume3
Issue number1
DOIs
StatePublished - Aug 1979

ASJC Scopus subject areas

  • Oncology
  • Toxicology
  • Pharmacology
  • Cancer Research
  • Pharmacology (medical)

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