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Updated: Oct 31, 2025
Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction
Published on: January 29, 2019
Targeted radionuclide therapy: an emerging field in solid tumours
Carlos Artigas1, Magdalena Mileva, Patrick Flamen
1Department of Nuclear Medicine, Institut Jules Bordet, Université Libre de Bruxelles (ULB), Brussels, Belgium.
Purpose Of Review:
Targeted radionuclide therapy (TRNT) is characterized by systemic administration of radiolabelled drugs, targeting specific molecular alterations expressed on the tumour cells. Small molecules, labelled with β- or α- emitting radioisotopes, are used to deliver radiation directly to the tumour sites. Pretreatment imaging to visualize whole body biodistribution of the target, using the same drugs labelled with positron or γ-emitting radionuclides, completes the concept of theranostic. This review will briefly summarize the current clinical research findings and applications of TRNT in solid tumours, mostly focusing on neuroendocrine and prostate neoplasms.
Recent Findings:
Peptide receptor radionuclide therapy is a major component in the management of gastroentropancreatic neuroendocrine tumours, with favourable safety profile, quality-of-life improvement and survival benefit. On the NETTER-1 study, it proved to be more effective than high-dose long-acting-release octreotide, leading to its regulatory approval. Prostate-specific membrane antigen (PSMA) is an excellent target for TRNT in prostate cancer. 177Lu-PSMA radioligand therapy demonstrated higher response rates in patients with metastatic castration resistant prostate cancer, when compared with second-line chemotherapy. New developments, including targeting of fibroblast activation proteins overexpressed in the tumour stroma, show promising preliminary results in the theranostic setting.
Summary:
Recent research has demonstrated and consolidated the use of TRNT against well established targets in neuroendocrine tumours and prostate cancer. The identification of new promising molecular targets for TRNT, will further expand the theranostic applications of radionuclides in the field of nuclear medicine.
Insights
Targeted radionuclide therapy (TRNT) offers a theranostic approach for solid tumors. This method uses radiolabeled drugs for precise tumor targeting, improving patient outcomes in neuroendocrine and prostate cancers.
Area of Science:
- Nuclear medicine
- Oncology
- Radiopharmaceutical therapy
Background:
- Targeted radionuclide therapy (TRNT) involves administering radiolabeled drugs to target specific molecular alterations on tumor cells.
- Small molecules labeled with beta or alpha-emitting radioisotopes deliver radiation directly to tumor sites.
- Theranostics combine therapeutic administration with pretreatment imaging using similar radiolabeled drugs.
Purpose of the Study:
- To review current clinical research findings and applications of TRNT in solid tumors.
- To focus on the use of TRNT in neuroendocrine and prostate neoplasms.
- To highlight the theranostic potential of radionuclide applications in nuclear medicine.
Main Methods:
- Systemic administration of radiolabeled drugs.
- Targeting specific molecular alterations on tumor cells.
- Pretreatment imaging for biodistribution assessment.
Main Results:
- Peptide receptor radionuclide therapy is key in managing neuroendocrine tumors, improving quality of life and survival.
- 177Lu-PSMA radioligand therapy shows high response rates in metastatic castration-resistant prostate cancer.
- Emerging targets like fibroblast activation proteins show promising theranostic results.
Conclusions:
- TRNT is established for neuroendocrine tumors and prostate cancer.
- New molecular targets will expand theranostic applications.
- TRNT enhances precision medicine in oncology.
