One of the problems of in vivo diagnosis and therapy of tumors with monoclonal antibodies is their heterogeneity with respect to antigen expression, with some cells expressing no antigen and others being weakly or strongly positive. Selected mixtures of antibodies to different antigens are therefore likely to react with more cells than single antibodies and be more effective for imaging and therapy. With this in mind, we have examined a new human colon cancer cell line (LIM1899) which has a heterogeneous expression of several cell surface molecules: by flow cytometry 38% were carcinoembryonic antigen positive; 64%, human milk fat globule positive, and 73%, CD46 positive; 87% of tumor cells bound a mixture of all three antibodies in vitro. Some blocking of the binding of anti-human milk fat globule antibody by the anti-CD46 antibody was noted. LIM1899 was established as a xenograft in nude mice and in vivo biodistribution studies performed using antibodies alone or in combination. Mixtures of antibodies clearly showed a higher percentage of injected dose of antibody in the tumor than did single antibodies: one antibody gave 10%; two together, 17 to 21%; and all three together gave 29% of the injected dose in the tumor. Tumor:blood ratios were also superior for combinations of antibodies, provided that low doses of the antibodies were used; at higher doses the effect was lost. The study demonstrates that combinations of antibodies are better than single antibodies for localization, provided that the dose used is carefully selected.

译文

用单克隆抗体对肿瘤进行体内诊断和治疗的问题之一是它们在抗原表达方面的异质性,其中一些细胞不表达抗原,而另一些细胞则呈弱阳性或强阳性。因此,针对不同抗原的抗体的选定混合物可能比单个抗体与更多的细胞反应,并且对成像和治疗更有效。考虑到这一点,我们检查了一种新的人结肠癌细胞系 (LIM1899),该细胞系具有几种细胞表面分子的异质表达: 通过流式细胞术,38% 为癌胚抗原阳性; 64%,人乳脂肪球阳性,73%,CD46阳性; 肿瘤细胞的87% 在体外结合所有三种抗体的混合物。注意到anti-CD46抗体对抗人乳脂肪球抗体结合的一些阻断。LIM1899被建立为裸鼠异种移植物,并单独或组合使用抗体进行体内生物分布研究。抗体混合物清楚地显示出肿瘤中注射抗体剂量的百分比高于单个抗体: 一种抗体产生10%; 两种在一起,17至21%; 并且所有三种一起产生肿瘤中注射剂量的29%。肿瘤: 如果使用低剂量的抗体,血液比率也优于抗体组合; 在较高剂量下,效果消失。研究表明,只要仔细选择使用的剂量,抗体的组合在定位方面优于单一抗体。

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