Radiolabeled imaging probes targeting angiogenesis for personalized medicine
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Updated: May 8, 2026

Preparing a 68Ga-labeled Arginine Glycine Aspartate (RGD)-peptide for Angiogenesis
Published on: January 7, 2019
Samantha Y A Terry, Mark Rijpkema, Keelara Abiraj
1Department of Nuclear Medicine, Radboud University Medical Centre Nijmegen, PO Box 9101, 6500 HB Nijmegen, The Netherlands. s.terry@nucmed.umcn.nl.
Abstract:
Angiogenesis is essential for tumor growth and inhibiting angiogenesis has become an important therapeutic strategy in clinical oncology. Nonetheless, the mechanisms behind anti-angiogenic therapeutics as well as resistance to these drugs remain unclear. With a lack of validated genetic or molecular biomarkers for anti-angiogenic responsiveness, novel methods to identify responsive patients are required. Non-invasive nuclear imaging would allow the elucidation of the basic drug mechanisms as well as resistance routes and aid the personalization of anti-angiogenic therapy by enabling target expression quantification prior to and during treatment. This review focuses on the development of radiolabeled probes to image four key proteins expressed during angiogenesis, namely vascular endothelial growth factor and its receptor, integrin αv β3, the extracellular domain of fibronectin and matrix metalloproteases, and how these probes can be utilized for personalized anti-angiogenic therapy.
Insights
Nuclear imaging with radiolabeled probes can identify patients who will respond to anti-angiogenic therapy. This approach helps understand drug mechanisms and resistance, personalizing cancer treatment.
Area of Science:
- Oncology
- Molecular Imaging
- Biomarker Development
Background:
- Angiogenesis is crucial for tumor growth, making anti-angiogenic therapy a key strategy in oncology.
- Mechanisms of anti-angiogenic drug action and resistance are not fully understood.
- Lack of biomarkers hinders patient selection for anti-angiogenic treatments.
Purpose of the Study:
- To review the development of radiolabeled probes for imaging key angiogenesis proteins.
- To explore the use of these probes in personalizing anti-angiogenic therapy.
- To elucidate drug mechanisms and resistance pathways non-invasively.
Main Methods:
- Development of radiolabeled probes targeting vascular endothelial growth factor (VEGF) and its receptor.
- Imaging integrin αvβ3, fibronectin, and matrix metalloproteases using nuclear imaging techniques.
- Quantification of target expression for patient stratification and treatment monitoring.
Main Results:
- Radiolabeled probes enable non-invasive imaging of angiogenesis markers.
- Imaging can reveal mechanisms of drug response and resistance.
- Personalized anti-angiogenic therapy can be facilitated through target expression quantification.
Conclusions:
- Non-invasive nuclear imaging offers a promising approach for personalized anti-angiogenic therapy.
- Radiolabeled probes can guide treatment decisions by assessing target engagement.
- Further development and validation of these probes are essential for clinical application.
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