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Updated: May 24, 2026

Development of a 68Gallium-Labeled D-Peptide PET Tracer for Imaging Programmed Death-Ligand 1 Expression
Published on: February 3, 2023
Radiolabelled peptides for oncological diagnosis
Peter Laverman1, Jane K Sosabowski, Otto C Boerman
1Department of Nuclear Medicine, Radboud University Nijmegen Medical Centre, Nijmegen, The Netherlands. P.Laverman@nucmed.umcn.nl
Abstract:
Radiolabelled receptor-binding peptides targeting receptors (over)expressed on tumour cells are widely under investigation for tumour diagnosis and therapy. The concept of using radiolabelled receptor-binding peptides to target receptor-expressing tissues in vivo has stimulated a large body of research in nuclear medicine. The (111)In-labelled somatostatin analogue octreotide (OctreoScan) is the most successful radiopeptide for tumour imaging, and was the first to be approved for diagnostic use. Based on the success of these studies, other receptor-targeting peptides such as cholecystokinin/gastrin analogues, glucagon-like peptide-1, bombesin (BN), chemokine receptor CXCR4 targeting peptides, and RGD peptides are currently under development or undergoing clinical trials. In this review, we discuss some of these peptides and their analogues, with regard to their potential for radionuclide imaging of tumours.
Insights
Radiolabeled peptides targeting tumor receptors show promise for cancer diagnosis and therapy. Octreotide is a successful example, with other peptides like bombesin and RGD peptides in development for imaging.
Area of Science:
- Nuclear medicine
- Oncology
- Radiopharmaceutical science
Background:
- Radiolabeled receptor-binding peptides are investigated for targeting tumors.
- The in vivo targeting of receptor-expressing tissues using radiolabeled peptides is a key area in nuclear medicine research.
- The (111)In-labeled somatostatin analogue octreotide (OctreoScan) is a leading radiopeptide for tumor imaging and the first approved diagnostic radiopeptide.
Purpose of the Study:
- To review various receptor-targeting peptides and their analogues.
- To discuss the potential of these peptides for radionuclide imaging of tumors.
Main Methods:
- Review of existing literature on radiolabeled peptides for tumor imaging.
- Discussion of specific peptide classes including somatostatin analogues, cholecystokinin/gastrin analogues, glucagon-like peptide-1, bombesin (BN), chemokine receptor CXCR4 targeting peptides, and RGD peptides.
Main Results:
- Octreotide (OctreoScan) is the most successful radiopeptide for tumor imaging to date.
- Several other receptor-targeting peptides are in development or clinical trials for diagnostic applications.
- These peptides target receptors overexpressed on tumor cells.
Conclusions:
- Radiolabeled peptides offer significant potential for the diagnosis and therapy of cancer.
- Ongoing research and clinical trials are expanding the range of available radiopeptides for nuclear medicine applications.
- The development of novel receptor-targeting peptides is crucial for advancing radionuclide tumor imaging.
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