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Published on: January 7, 2019
Candidates for peptide receptor radiotherapy today and in the future
Jean Claude Reubi1, Helmut R Mäcke, Eric P Krenning
1Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Berne, Switzerland. reubi@pathology.unibe.ch
Abstract:
Regulatory peptide receptors are overexpressed in numerous human cancers. These receptors have been used as molecular targets by which radiolabeled peptides can localize cancers in vivo and, more recently, to treat cancers with peptide receptor radiation therapy (PRRT). This review describes the candidate tumors eligible for such radiotherapy on the basis of their peptide receptor content and discusses factors in PRRT eligibility. At the present time, PRRT is performed primarily with somatostatin receptor- and cholecystokinin-2 (CCK2)-receptor-expressing neuroendocrine tumors with radiolabeled octreotide analogs or with radiolabeled CCK2-selective analogs. In the future, PRRT may be extended to many other tumor types, including breast, prostate, gut, pancreas, and brain tumors, that have recently been shown to overexpress several other peptide receptors, such as gastrin-releasing peptide-, neurotensin-, substance P-, glucagon-like peptide 1-, neuropeptide Y-, or corticotropin-releasing factor-receptors. A wide range of radiolabeled peptides is being developed for clinical use. Improved somatostatin or CCK(2) analogs as well as newly designed bombesin, neurotensin, substance P, neuropeptide Y, and glucagon-like peptide-1 analogs offer promise for future PRRT.
Insights
Peptide receptor radiation therapy (PRRT) targets overexpressed receptors in cancers. Future applications may expand PRRT to various tumor types using novel radiolabeled peptides.
Area of Science:
- Oncology
- Nuclear Medicine
- Molecular Imaging
Background:
- Regulatory peptide receptors are frequently overexpressed in various human cancers.
- These receptors serve as molecular targets for cancer detection and therapy.
- Peptide receptor radiation therapy (PRRT) utilizes radiolabeled peptides to target cancer cells.
Purpose of the Study:
- To review candidate tumors eligible for PRRT based on peptide receptor expression.
- To discuss factors influencing patient eligibility for PRRT.
- To explore the potential of novel radiolabeled peptides for future PRRT applications.
Main Methods:
- Review of current literature on peptide receptor expression in tumors.
- Analysis of factors determining PRRT eligibility.
- Overview of existing and emerging radiolabeled peptides for PRRT.
Main Results:
- PRRT is currently used for neuroendocrine tumors expressing somatostatin or cholecystokinin-2 (CCK2) receptors.
- Future PRRT may include breast, prostate, gut, pancreas, and brain tumors overexpressing various peptide receptors.
- Development of new analogs for somatostatin, CCK2, bombesin, neurotensin, substance P, neuropeptide Y, and glucagon-like peptide-1 is ongoing.
Conclusions:
- PRRT is an established therapy for specific neuroendocrine tumors.
- Expanding PRRT to other cancer types is feasible due to the identification of novel peptide receptor targets.
- Advancements in radiolabeled peptide development hold significant promise for the future of PRRT.
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