Development of 177Lu-nanobodies for radioimmunotherapy of HER2-positive breast cancer: evaluation of different bifunctional chelators

被引：74

作者：

D'Huyvetter, Matthias ^{[1
,2
]}

Aerts, An ^{[2
]}

Xavier, Catarina ^{[1
]}

Vaneycken, Ilse ^{[1
]}

Devoogdt, Nick ^{[1
]}

Gijs, Marlies ^{[2
]}

Impens, Nathalie ^{[2
]}

Baatout, Sarah ^{[2
]}

Ponsard, Bernard ^{[3
]}

Muyldermans, Serge ^{[4
,5
]}

Caveliers, Vicky ^{[1
,6
]}

Lahoutte, Tony ^{[1
,6
]}

机构：

[1] Vrije Univ Brussel, Vivo Cellular & Mol Imaging Lab, Brussels, Belgium

[2] Belgian Nucl Res Ctr SCK CEN, Radiobiol Unit, Mol & Cellular Biol Expert Grp, Mol, Belgium

[3] Belgian Nucl Res Ctr SCK CEN, Radioisotopes & Silicon Prod Unit, Belgian Reactor Expert Grp 2, Mol, Belgium

[4] Vlaams Inst Biotechnol, Dept Mol & Cell Interact, Brussels, Belgium

[5] Vrije Univ Brussel, Dept Cellular & Mol Immunol, Brussels, Belgium

[6] UZ Brussel, Dept Nucl Med, Brussels, Belgium

来源：

CONTRAST MEDIA & MOLECULAR IMAGING | 2012年 / 7卷 / 02期

关键词：

HER2; Lutetium-177; nanobody; breast cancer; bifunctional chelator; LU-177; ANTIBODIES; NANOBODIES; HER-2; MICE;

D O I：

10.1002/cmmi.491

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

100231 [临床病理学]; 100902 [航空航天医学];

摘要：

Nanobodies show favourable pharmacokinetic characteristics for tumor targeting, including high tumor-to-background-ratios. Labelled with a therapeutic radionuclide, nanobodies could be used as an adjuvant treatment option for HER2-overexpressing minimal residual disease. The therapeutic radionuclide Lutetium-177 is linked to the nanobody using a bifunctional chelator. The choice of the bifunctional chelator could affect the in vivo behaviour of the radiolabeled nanobody. Consequently, we compared four different bifunctional chelators - p-SCN-Bn-DOTA, DOTA-NHS-ester, CHX-A-DTPA or 1B4M-DTPA - in order to select the optimal chemical link between Lutetium-177 and a HER2 targeting nanobody.

引用

页码：254 / 264

页数：11

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