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Pharmaceuticals 2014, 7(3), 311-338; doi:10.3390/ph7030311
Review

Radiolabeled Cetuximab Conjugates for EGFR Targeted Cancer Diagnostics and Therapy

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Received: 20 December 2013; in revised form: 11 February 2014 / Accepted: 21 February 2014 / Published: 5 March 2014
(This article belongs to the Special Issue Radiopharmaceutical Chemistry between Imaging and Radioendotherapy)
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Abstract: The epidermal growth factor receptor (EGFR) has evolved over years into a main molecular target for the treatment of different cancer entities. In this regard, the anti-EGFR antibody cetuximab has been approved alone or in combination with: (a) chemotherapy for treatment of colorectal and head and neck squamous cell carcinoma and (b) with external radiotherapy for treatment of head and neck squamous cell carcinoma. The conjugation of radionuclides to cetuximab in combination with the specific targeting properties of this antibody might increase its therapeutic efficiency. This review article gives an overview of the preclinical studies that have been performed with radiolabeled cetuximab for imaging and/or treatment of different tumor models. A particularly promising approach seems to be the treatment with therapeutic radionuclide-labeled cetuximab in combination with external radiotherapy. Present data support an important impact of the tumor micromilieu on treatment response that needs to be further validated in patients. Another important challenge is the reduction of nonspecific uptake of the radioactive substance in metabolic organs like liver and radiosensitive organs like bone marrow and kidneys. Overall, the integration of diagnosis, treatment and monitoring as a theranostic approach appears to be a promising strategy for improvement of individualized cancer treatment.
Keywords: EGFR; radiolabeled cetuximab conjugates; radioimmunotherapy (RIT); cancer theranostics; external beam radiotherapy (EBRT); endoradionuclide therapy EGFR; radiolabeled cetuximab conjugates; radioimmunotherapy (RIT); cancer theranostics; external beam radiotherapy (EBRT); endoradionuclide therapy
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Sihver, W.; Pietzsch, J.; Krause, M.; Baumann, M.; Steinbach, J.; Pietzsch, H.-J. Radiolabeled Cetuximab Conjugates for EGFR Targeted Cancer Diagnostics and Therapy. Pharmaceuticals 2014, 7, 311-338.

AMA Style

Sihver W, Pietzsch J, Krause M, Baumann M, Steinbach J, Pietzsch H-J. Radiolabeled Cetuximab Conjugates for EGFR Targeted Cancer Diagnostics and Therapy. Pharmaceuticals. 2014; 7(3):311-338.

Chicago/Turabian Style

Sihver, Wiebke; Pietzsch, Jens; Krause, Mechthild; Baumann, Michael; Steinbach, Jörg; Pietzsch, Hans-Jürgen. 2014. "Radiolabeled Cetuximab Conjugates for EGFR Targeted Cancer Diagnostics and Therapy." Pharmaceuticals 7, no. 3: 311-338.



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