Clinical Evaluation of Radio-Labelled Bleomycin for Tumor Detection

Investigations with bleomycin labelled with radionuclides other than ⁵⁷Co in patients with cancer and in tumor-bearing animals are described. In patients ⁵⁷Co-bleo appears to be a better tumor-seeking radiopharmaceutical than ¹¹¹In-bleo, ^99mTc-bleo or ¹⁹⁷Hg-bleo. This can be explained by a higher stability in vivo and a better tumor-seeking property of ⁵⁷Co-bleo and less disturbing activity in the cardiac pool and in bone and other normal tissues when assessing the scintigram.

Results with ¹¹¹In-bleo labelled in acidic solution are not essentially different from those with ¹¹¹In-bleo labelled in neutral solution.

Results of ¹⁹⁷Hg-bleo are almost identical with those of ¹⁹⁷HgCl₂ regarding the tumor-seeking effect as well as the distribution in normal tissues and organs. Probably the complex of ¹⁹⁷Hg to bleomycin is not stable in vivo. The superiority of ⁵⁷Co-bleo over ^99mTc-bleo, ¹⁹⁷Hg-bleo and also over ⁶⁷Cu-bleo is confirmed by experiments on tumor bearing animals.

We may conclude that the indication for use of bleomycin as a tumor-seeking pharmaceutical labelled with ¹¹¹In, ^99mTc, ¹⁹⁷Hg or ⁶⁷Cu seems to be very limited.

Es werden klinische und tierexperimentelle Verteilungsstudien mit ⁵⁷Co-, ¹¹¹In-, ^99mTc-, ¹⁹⁷Hg- und ⁶⁷Cu-Bleomycin beschrieben.

Bei Patienten zeigte sich, daß ⁵⁷Co-Bleo als Radiopharmakon in der Tumorszintigraphie den Präparaten ¹¹¹In-Bleo, ^99mTc-Bleo oder ¹⁹⁷Hg-Bleo überlegen ist. Die Ursache ist eine größere Stabilität in vivo und bessere Eigenschaften des ⁵⁷Co-Bleo zum Nachweis von Tumoren und eine in der Beurteilung des Szintigramms weniger störende Radioaktivität im Herzpool und in den Knochen und anderen normalen Geweben.

Die Resultate mit in sauren Lösungen markiertem ¹¹¹In-Bleo sind von denen mit in neutralen Lösungen markiertem ¹¹¹In-Bleo nicht wesentlich verschieden.

Die Ergebnisse mit ¹⁹⁷Hg-Bleo sind fast identisch mit denen mit ¹⁹⁷Hg Cl₂ sowohl im „Tumor-Nachweis-Effekt” als auch in der Verteilung in normalen Geweben und Organen. Wahrscheinlich ist in vivo der Komplex von ¹⁹⁷Hg mit Bleomycin nicht stabil.

⁵⁷Co-Bleo ist ^99mTc-Bleo, ¹⁹⁷Hg-Bleo und auch ⁶⁷Cu-Bleo überlegen, wie durch Experimente bei Tieren mit Tumoren bestätigt wird.

Dies führt zum Schluß, daß die Indikation zur Verwendung von Bleomycin als mit ¹¹¹In, ^99mTc oder ¹⁹⁷Hg markiertes Pharmakon zum Nachweis von Tumoren begrenzt ist.

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