Radiolabelled Regulatory Peptides for Imaging and Therapy

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Radiolabelled Regulatory Peptides for Imaging and Therapy

Anti-Cancer Agents in Medicinal Chemistry, 7(3): 345-357.

Author(s): M. de Jong, T. J. Visser, E. de Blois, W. A. P. Breeman, D. J. Kwekkeboom and E P Krenning.

Affiliation: Erasmus MC Rotterdam,University Medical Center Rotterdam, Department of Nuclear Medicine, Dr.Molewaterplein 40, 3015 GD Rotterdam, The Netherlands.


Radiolabelled peptides have shown to be an important class of radiopharmaceuticals for imaging and therapy of malignancies expressing receptors of regulatory peptides. These peptides have high affinity and specificity for their receptors. The majority of these receptors are present at different levels in different tissues and tumours. This review focuses on the application of regulatory peptides radiolabelled with 67/68Ga , 90Y, 111In or 177Lu. Due attention is given to the current status of research, limitations and future perspectives of the application of these radiolabelled peptides for imaging and radiotherapy. It also covers elements of the basic science and preclinical and clinical aspects in general, however, mostly based on somatostatin receptor-mediated imaging and therapy. New analogues, chelators, radionuclides and combinations thereof are discussed.


somatostatin, scintigraphy, peptide receptor-targeted radiotherapy, radiolabelling, DTPA, DOTA, receptor, gastrin-releasing peptide, bombesin, substance P.

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Article Details

Volume: 7
Issue Number: 3
First Page: 345
Last Page: 357
Page Count: 13
DOI: 10.2174/187152007780618171
Price: $58
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