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Evaluation of Radioactive Compounds for the External Detection of Cerebral Tumors^*

( Division of Neurological Surgery and Department of Radiology, The Johns Hopkins Hospital and University, Baltimore, Maryland; and Laboratory of Technical Development, National Heart Institute, Bethesda, Maryland)

Studies of the distribution in the organs and body fluids of various radioactive compounds in a pure strain of tumor-bearing mice indicated the potential value of serum albumin-I¹³¹, Cholografin-I¹³¹, Neohydrin-Hg²⁰³, and cobaltous-Co⁵⁷ tetraphenylporphinesulfonate for brain tumor localization in man. For serum albumin-I¹³¹, the tumor concentration was higher than for several substances tested, and the optimum tumor-to-brain concentration ratio was 33 to 1. A persistently high blood level and a relatively long biological half-life were its chief disadvantages.

Neohydrin-Hg²⁰³ and Cholografin-I¹³¹ were removed from the blood stream more quickly than albumin-I¹³¹, and their total-body biological half-lives were considerably shorter; tumor-to-brain concentration ratios in mice were 22 to 1 and 80 to 1, respectively. The absolute tumor concentrations were lower than for serum albumin and were especially low for Cholografin-I¹³¹.

Cobaltous-Co⁵⁷ tetraphenylporphinesulfonate produced absolute tumor concentrations as high as did albumin-I¹³¹, and the tumor-to-brain concentration ratios were 60 to 1. Moreover, the blood levels after 24 hours were considerably lower than for albumin-I¹³¹.

All substances evaluated which produced high tumor-to-brain concentration ratios were protein-bound in the plasma. Free radioactive ions and positron-emitting compounds which have been used for clinical studies to date gave tumor-to-brain concentration ratios inferior to protein-bound substances.

^* This work was supported by Grant #A-3128, U.S.P.H.S., National Institutes of Health, by a Special Fellowship (BT-764) from the National Institute of Neurological Diseases and Blindness, Public Health Service, and by Institutional Grants from the American Cancer Society.

Received 6/29/62.