^<131>I-diethylstibestrol diphosphateの研究 : その生体内分布と前立腺scanningの可能性について

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Diethylstilbestrol diphosphate which has been in wide use for cancer of the prostate is said to change to active form (stilbestrol) by acid phosphatase. Tubis et al. (1967) suggested probability of scintiscanning of the prostate gland by ^<131>I labeled diethylstilbestrol diphosphate. Yet there has been no literature on this subject. This paper deals with results of animal experiment and clinical studies with this drug. Fifty five μCi of ^<131>I labeled diethylstilbestrol diphosphate for each rat was administered by the tail vein. Specific activity of ^<131>I labeled diethylstilbestrol diphosphate was 67 μCi per mg. Each group of this experiment consisted of 3 male rats weighing 110-150 g. Radioactivities of each organ (prostate, liver, kidney, spleen, heart, lung, intestine, adrenal and testicle) were determined in different time intervals (5, 15, 30, 60 min., 3, 6, 12, 24 hr., 2, 3, 5, 7 day) and the relative specific activity (R.S.A.) of each organ was computed. The highest concentration was observed in the liver followed by the kidney, and a relatively long retension was recognized in the liver. The R.S.A. in the prostate was demonstrated to be lower than expected (Table 1). In clinical studies on 10 patients (7 prostatic cancer, 1 prostatitis, 1 bladder tumor and 1 chronic cystitis), 500 μCi of ^<131>I labeled diethylstilbestrol diphosphate was administered intravenously. The uptake by each organ was in the same order as described in the rats, and the uptake by prostatic cancer and its metastatic lesion was not so large as expected. The scintigram of the prostate gland was not depicted. In rabbit experiment the prostatic concentration of ^<131>I labeled diethylstilbestrol diphosphate was 0.03-0.04% of the administered dose (56 μCi/kg) in 3 hours. Prior administration of non labeled diethylstilbestrol diphosphate (71.4 mg/kg) did not alter this radioactive concentration level.
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^<131>I-diethylstibestrol diphosphateの研究 : その生体内分布と前立腺scanningの可能性について

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