Radiolabeled imaging probes targeting angiogenesis for personalized medicine

S. Terry, M. Rijpkema, K. Abiraj, W. van der Graaf, W. Oyen and O. Boerman

Department of Nuclear Medicine, Radboud University Medical Centre Nijmegen, PO Box 9101, 6500 HB Nijmegen, The Netherlands.


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.