Synthesis and evaluation of a macrocyclic bifunctional chelating agent for use with bismuth radionuclides

被引：23

作者：

Garmestani, K

Yao, Z

Zhang, M

Wong, K

Park, CW

Pastan, I

Carrasquillo, JA

Brechbiel, MW

机构：

[1] NCI, Radioimmune & Inorgan Chem Sect, ROB, DCS, Bethesda, MD 20892 USA

[2] NCI, Ctr Clin, Dept Nucl Med, NIH, Bethesda, MD 20892 USA

[3] NCI, DCS, Metab Branch, NIH, Bethesda, MD 20892 USA

[4] NCI, DBS, Mol Biol Lab, NIH, Bethesda, MD 20892 USA

来源：

NUCLEAR MEDICINE AND BIOLOGY | 2001年 / 28卷 / 04期

关键词：

bismuth; Bi-205; Bi-206; radioimmunotherapy; bifunctional chelating agent; alpha-therapy;

D O I：

10.1016/S0969-8051(00)00203-1

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

1002 ; 100207 ; 1009 ;

摘要：

The detailed synthesis of the bifunctional chelating agent 2-(p-isothiocyanatobenzyl)-1,4,7,10,13-pentaazacyclopentadecane-N,N',N",N"',N""-pentaacetic acid (BF_PEPA) is reported. This ligand was conjugated to monoclonal antibody B3 and the resultant immunoconjugate radiolabeled with Bi-205,Bi-206. The in vivo stability of the radiolabeled immunoconjugate, and targeting characteristics were determined by biodistribution studies in A431 xenograft tumor-bearing mice sacrificed at 0.5, 1, 2, 4, and 24 hr. Results indicate that BF_PEPA appears to not be a suitable bifunctional chelating agent for sequestering isotopes of Bi(III) for radioimmunotherapy applications. (C) 2001 Elsevier Science Inc. All rights reserved.

引用

页码：409 / 418

页数：10

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