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单克隆抗体B72.3及其用125I或111In标记的片段的药代动力学

Pharmacokinetics of the monoclonal antibody B72.3 and its fragments labeled with either 125I or 111In.

作者信息

Brown B A, Comeau R D, Jones P L, Liberatore F A, Neacy W P, Sands H, Gallagher B M

出版信息

Cancer Res. 1987 Feb 15;47(4):1149-54.

PMID:3802096
Abstract

A comparison of the pharmacokinetics of intact B72.3 (a murine monoclonal antibody specific for human breast and colon carcinoma) with F(ab')2 and Fab fragments labeled with 111In and 125I was done in athymic mice bearing target (LS174T) and non-target (HCT-15) tumors. IgG B72.3 labeled with either isotype imaged LS174T. Biodistributions of both labels were similar in all organs except liver. F(ab')2 also imaged the LS174T tumor, while Fab bearing either isotype did not. The blood clearance was Fab greater than F(ab')2 greater than immunoglobulin G B72.3 for both isotopes. 111In-labeled fragments yielded large accumulations in the kidneys which persisted for 2 days. The different patterns of biodistribution for the various forms of B72.3 labeled with the two isotopes suggest that the most desirable combination of fragment and isotope will depend on the intended use.

摘要

在携带靶标(LS174T)和非靶标(HCT - 15)肿瘤的无胸腺小鼠中,对完整的B72.3(一种针对人乳腺癌和结肠癌的鼠单克隆抗体)与用111In和125I标记的F(ab')2和Fab片段的药代动力学进行了比较。用同型抗体标记的IgG B72.3对LS174T进行了成像。除肝脏外,两种标记物在所有器官中的生物分布相似。F(ab')2也对LS174T肿瘤进行了成像,而携带任何一种同型抗体的Fab则未成像。两种同位素的血液清除率均为Fab大于F(ab')2大于免疫球蛋白G B72.3。111In标记的片段在肾脏中大量蓄积并持续2天。用两种同位素标记的各种形式的B72.3的不同生物分布模式表明,片段和同位素的最理想组合将取决于预期用途。

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