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First published online August 17, 2007, 10.2967/jnumed.107.040816
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Journal of Nuclear Medicine Vol. 48 No. 9 1536-1544
© 2007 by Society of Nuclear Medicine
doi: 10.2967/jnumed.107.040816

Basic Science Investigation

microPET of Tumor Integrin {alpha}vß3 Expression Using 18F-Labeled PEGylated Tetrameric RGD Peptide (18F-FPRGD4)

Zhanhong Wu*,1,2, Zi-Bo Li*,1, Kai Chen1, Weibo Cai1, Lina He1, Frederick T. Chin1, Fang Li2 and Xiaoyuan Chen1

1 The Molecular Imaging Program at Stanford (MIPS), Department of Radiology and Bio-X Program, Stanford University School of Medicine, Stanford, California; and 2 Department of Nuclear Medicine, Peking Union Medical College Hospital, Beijing, China

Correspondence: For correspondence or reprints contact: Xiaoyuan Chen, PhD, The Molecular Imaging Program at Stanford (MIPS), Department of Radiology and Bio-X Program, Stanford University School of Medicine, 1201 Welch Rd., P095, Stanford, CA 94305-5484. E-mail: shawchen{at}stanford.edu

In vivo imaging of {alpha}vß3 expression has important diagnostic and therapeutic applications. Multimeric cyclic RGD peptides are capable of improving the integrin {alpha}vß3–binding affinity due to the polyvalency effect. Here we report an example of 18F-labeled tetrameric RGD peptide for PET of {alpha}vß3 expression in both xenograft and spontaneous tumor models. Methods: The tetrameric RGD peptide E{E[c(RGDyK)]2}2 was derived with amino-3,6,9-trioxaundecanoic acid (mini-PEG; PEG is poly(ethylene glycol)) linker through the glutamate {alpha}-amino group. NH2-mini-PEG-E{E[c(RGDyK)]2}2 (PRGD4) was labeled with 18F via the N-succinimidyl-4-18F-fluorobenzoate (18F-SFB) prosthetic group. The receptor-binding characteristics of the tetrameric RGD peptide tracer 18F-FPRGD4 were evaluated in vitro by a cell-binding assay and in vivo by quantitative microPET imaging studies. Results: The decay-corrected radiochemical yield for 18F-FPRGD4 was about 15%, with a total reaction time of 180 min starting from 18F-F–. The PEGylation had minimal effect on integrin-binding affinity of the RGD peptide. 18F-FPRGD4 has significantly higher tumor uptake compared with monomeric and dimeric RGD peptide tracer analogs. The receptor specificity of 18F-FPRGD4 in vivo was confirmed by effective blocking of the uptake in both tumors and normal organs or tissues with excess c(RGDyK). Conclusion: The tetrameric RGD peptide tracer 18F-FPRGD4 possessing high integrin-binding affinity and favorable biokinetics is a promising tracer for PET of integrin {alpha}vß3 expression in cancer and other angiogenesis related diseases.

Key Words: microPET • integrin {alpha}vß3 • tetrameric RGD peptide • PEGylation • 18F

* Contributed equally to this work.

COPYRIGHT © 2007 by the Society of Nuclear Medicine, Inc.


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