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Updated: Jul 15, 2026

Harnessing the Bioorthogonal Inverse Electron Demand Diels-Alder Cycloaddition for Pretargeted PET Imaging
Published on: February 3, 2015
Targeted therapy in nuclear medicine--current status and future prospects
W J G Oyen1, L Bodei, F Giammarile
1Therapy Committee of the European Association of Nuclear Medicine, Hollandstrasse 14 / Mezzanine, A-1020 Vienna, Austria. w.oyen@nucmed.umcn.nl
Abstract:
In recent years, a number of new developments in targeted therapies using radiolabeled compounds have emerged. New developments and insights in radioiodine treatment of thyroid cancer, treatment of lymphoma and solid tumors with radiolabeled monoclonal antibodies (mAbs), the developments in the application of radiolabeled small receptor-specific molecules such as meta-iodobenzylguanidine and peptides and the position of locoregional treatment in malignant involvement of the liver are reviewed. The introduction of recombinant human thyroid-stimulating hormone and the possibility to enhance iodine uptake with retinoids has changed the radioiodine treatment protocol of patients with thyroid cancer. Introduction of radiolabeled mAbs has provided additional treatment options in patients with malignant lymphoma, while a similar approach proves to be cumbersome in patients with solid tumors. With radiolabeled small molecules that target specific receptors on tumor cells, high radiation doses can be directed to tumors in patients with disseminated disease. Radiolabeled somatostatin derivatives for the treatment of neuroendocrine tumors are the role model for this approach. Locoregional treatment with radiopharmaceuticals of patients with hepatocellular carcinoma or metastases to the liver may be used in inoperable cases, but may also be of benefit in a neo-adjuvant or adjuvant setting. Significant developments in the application of targeted radionuclide therapy have taken place. New treatment modalities have been introduced in the clinic. The concept of combining therapeutic radiopharmaceuticals with other treatment modalities is more extensively explored.
Insights
Targeted radionuclide therapy has advanced significantly, offering new options for thyroid cancer, lymphoma, and solid tumors using radiolabeled compounds. These targeted therapies, including antibodies and small molecules, are improving treatment for various cancers.
Area of Science:
- Oncology
- Nuclear Medicine
- Radiopharmaceutical Therapy
Background:
- Targeted radionuclide therapy has seen significant advancements.
- New developments include radioiodine treatment, radiolabeled monoclonal antibodies (mAbs), and small receptor-specific molecules.
Purpose of the Study:
- To review recent developments in targeted therapies using radiolabeled compounds.
- To discuss the application of these therapies in various cancers, including thyroid cancer, lymphoma, and solid tumors.
- To explore locoregional treatment for liver malignancies.
Main Methods:
- Review of current literature on targeted radionuclide therapy.
- Discussion of specific radiolabeled agents like radioiodine, mAbs, meta-iodobenzylguanidine, peptides, and somatostatin derivatives.
- Analysis of treatment protocols and outcomes for different cancer types.
Main Results:
- Radioiodine treatment protocols for thyroid cancer have been updated with recombinant human thyroid-stimulating hormone and retinoids.
- Radiolabeled mAbs offer new options for lymphoma but are challenging for solid tumors.
- Radiolabeled small molecules and peptides enable high-dose radiation delivery to disseminated tumors, with somatostatin derivatives as a model.
- Locoregional radiopharmaceutical treatment is effective for inoperable liver cancers and can be used in neoadjuvant/adjuvant settings.
Conclusions:
- Targeted radionuclide therapy has significantly advanced, with new clinical modalities introduced.
- Combining therapeutic radiopharmaceuticals with other treatment modalities is an area of increasing exploration.
- These developments offer improved treatment strategies for various malignancies.
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