Pimm M V, Perkins A C, Baldwin R W
Eur J Nucl Med. 1985;11(8):300-4. doi: 10.1007/BF00252341.
The blood, tumour and whole-body levels and survivals of 131I- and 111In-labelled monoclonal antibody (791T/36) have been compared in mice with human tumour xenografts. The blood levels and survivals of 131I- and 111In-labelled antibody were similar when expressed as proportions of the injected doses. However, the whole-body survival of 111In following administration of 111In-labelled antibody was over twice as long as that of 131I after administration of 131I-labelled antibody, principally because free 131I was rapidly excreted but free 111In was retained, primarily in liver, spleen and kidneys. Consequently, when expressed in relation to the whole body, blood levels of 111In became progressively lower than those of 131I following administration of labelled antibodies. In mice with human tumour xenografts the proportion of the injected dose of 111In from 111In-labelled antibody deposited in tumour tissue was 4-5 times higher than that of 131I from 131I-labelled antibody. When compared with the whole-body levels of radiolabel the difference was less marked, although 111In accumulation in tumour was more rapid. The higher levels and longer retention of 111In in tumour produced tumour-to-blood ratios that were 7-8 times those achieved with 131I-labelled antibody.
在患有人类肿瘤异种移植的小鼠中,对¹³¹I和¹¹¹In标记的单克隆抗体(791T/36)的血液、肿瘤及全身水平和存留情况进行了比较。当以注射剂量的比例表示时,¹³¹I和¹¹¹In标记抗体的血液水平和存留情况相似。然而,注射¹¹¹In标记抗体后¹¹¹In的全身存留时间是注射¹³¹I标记抗体后¹³¹I的两倍多,主要是因为游离¹³¹I迅速排出,而游离¹¹¹In被保留,主要在肝脏、脾脏和肾脏中。因此,与全身相比,注射标记抗体后¹¹¹In的血液水平逐渐低于¹³¹I的血液水平。在患有人类肿瘤异种移植的小鼠中,¹¹¹In标记抗体中¹¹¹In注射剂量沉积在肿瘤组织中的比例比¹³¹I标记抗体中¹³¹I的比例高4至5倍。与放射性标记的全身水平相比,差异不太明显,尽管¹¹¹In在肿瘤中的积累更快。¹¹¹In在肿瘤中的较高水平和较长存留时间产生的肿瘤与血液的比率是¹³¹I标记抗体所达到比率的7至8倍。