Theranostics 2016; 6(1):78-92. doi:10.7150/thno.13242 This issue


Clinical Application of Radiolabeled RGD Peptides for PET Imaging of Integrin αvβ3

Haojun Chen1,2, Gang Niu2✉, Hua Wu1✉, Xiaoyuan Chen2✉

1. Department of Nuclear Medicine, Xiamen Cancer Center, the First Affiliated Hospital of Xiamen University, Xiamen, China
2. Laboratory of Molecular Imaging and Nanomedicine, National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health, Bethesda, Maryland

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Chen H, Niu G, Wu H, Chen X. Clinical Application of Radiolabeled RGD Peptides for PET Imaging of Integrin αvβ3. Theranostics 2016; 6(1):78-92. doi:10.7150/thno.13242. Available from

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Molecular imaging for non-invasive assessment of angiogenesisis is of great interest for clinicians because of the wide-spread application of anti-angiogenic cancer therapeutics. Besides, many other interventions that involve the change of blood vessel/tumor microenvironment would also benefit from such imaging strategies. Of the imaging techniques that target angiogenesis, radiolabeled Arg-Gly-Asp (RGD) peptides have been a major focus because of their high affinity and selectivity for integrin αvβ3--one of the most extensively examined target of angiogenesis. Since the level of integrin αvβ3 expression has been established as a surrogate marker of angiogenic activity, imaging αvβ3 expression can potentially be used as an early indicator of effectiveness of antiangiogenic therapy at the molecular level. In this review, we summarize RGD-based PET tracers that have already been used in clinical trials and intercompared them in terms of radiosynthesis, dosimetry, pharmacokinetics and clinical applications. A perspective of their future use in the clinic is also provided.

Keywords: Angiogenesis, RGD, PET, clinical translation