Beaumier P L, Krohn K A, Carrasquillo J A, Eary J, Hellström I, Hellström K E, Nelp W B, Larson S M
J Nucl Med. 1985 Oct;26(10):1172-9.
The tumor targeting capacity of monoclonal antibody Fab fragments was explored in nude mice bearing human melanoma xenografts. Radioiodinated Fab 8.2 and 96.5, specific for melanoma-associated antigen p97, were tested in vitro for immunoreactivity and in vivo for tumor localization relative to a co-administered control, Fab 1.4. Fab was cleared rapidly from the blood with a T1/2 of 3-3.5 hr and greater than 90% of the injected radioactivity was excreted by 16 hr. The mean specific Fab in tumor reached a maximum of 3.5% injected dose/g at 4 hr and decreased to 1.5% at 16 hr. Over the same period, the ratio of specific/control Fab in tumor normalized to blood, the localization index, rose from 3 to 25 compared with ratios near unity for all other tissues. The concentration of specific Fab in tumor could be correlated to the amount of Fab protein administered as well as its immunoreactivity.
在携带人黑色素瘤异种移植瘤的裸鼠中研究了单克隆抗体Fab片段的肿瘤靶向能力。针对黑色素瘤相关抗原p97的放射性碘化Fab 8.2和96.5,在体外测试其免疫反应性,在体内测试相对于共同给药的对照Fab 1.4的肿瘤定位。Fab从血液中迅速清除,半衰期为3-3.5小时,超过90%的注入放射性在16小时内排出。肿瘤中的平均特异性Fab在4小时时达到最大注入剂量/克的3.5%,在16小时时降至1.5%。在同一时期,肿瘤中特异性/对照Fab与血液的归一化比值,即定位指数,从3上升到25,而所有其他组织的比值接近1。肿瘤中特异性Fab的浓度与给药的Fab蛋白量及其免疫反应性相关。