Rasker J J, Beekhuis H, van de Poll M A, Versluis A, Jurjens H, Woldring M G
Nuklearmedizin. 1978 Dec;17(6):238-48.
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.
本文描述了用除57Co以外的放射性核素标记博来霉素,在癌症患者和荷瘤动物中进行的研究。在患者中,57Co标记的博来霉素似乎比111In标记的博来霉素、99mTc标记的博来霉素或197Hg标记的博来霉素是更好的肿瘤定位放射性药物。这可以通过57Co标记的博来霉素在体内具有更高的稳定性和更好的肿瘤定位特性来解释,并且在评估闪烁图时,心脏血池、骨骼和其他正常组织中的干扰活性较小。在酸性溶液中标记的111In标记的博来霉素的结果与在中性溶液中标记的111In标记的博来霉素的结果没有本质区别。197Hg标记的博来霉素在肿瘤定位效果以及在正常组织和器官中的分布方面的结果与197HgCl2几乎相同。可能197Hg与博来霉素的复合物在体内不稳定。在荷瘤动物实验中证实了57Co标记的博来霉素优于99mTc标记的博来霉素、197Hg标记的博来霉素以及67Cu标记的博来霉素。我们可以得出结论,使用111In、99mTc、197Hg或67Cu标记的博来霉素作为肿瘤定位药物的适应证似乎非常有限。