BioSpace Collaborative - Quantitative Analysis and Comparison Study of [18F]AlF-NOTA-PRGD2, [18F]FPPRGD2 and [68Ga]Ga-NOTA-PRGD2 Using a Reference Tissue Model

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Biochemistry - Biotechnology - Chemistry - Neuroscience - Non-Clinical Medicine - Radiology and Medical Imaging

Quantitative Analysis and Comparison Study of [18F]AlF-NOTA-PRGD2, [18F]FPPRGD2 and [68Ga]Ga-NOTA-PRGD2 Using a Reference Tissue Model
Published: Friday, May 18, 2012
Author: Ning Guo et al.

by Ning Guo, Lixin Lang, Weihua Li, Dale O. Kiesewetter, Haokao Gao, Gang Niu, Qingguo Xie, Xiaoyuan Chen

With favorable pharmacokinetics and binding affinity for a_vß₃ integrin, ¹⁸F-labeled dimeric cyclic RGD peptide ([¹⁸F]FPPRGD2) has been intensively used as a PET imaging probe for lesion detection and therapy response monitoring. A recently introduced kit formulation method, which uses an ¹⁸F-fluoride-aluminum complex labeled RGD tracer ([¹⁸F]AlF-NOTA-PRGD2), provides a strategy for simplifying the labeling procedure to facilitate clinical translation. Meanwhile, an easy-to-prepare ⁶⁸Ga-labeled NOTA-PRGD2 has also been reported to have promising properties for imaging integrin a_vß₃. The purpose of this study is to quantitatively compare the pharmacokinetic parameters of [¹⁸F]FPPRGD2, [¹⁸F]AlF-NOTA-PRGD2, and [⁶⁸Ga]Ga-NOTA-PRGD2. U87MG tumor-bearing mice underwent 60-min dynamic PET scans following the injection of three tracers. Kinetic parameters were calculated using Logan graphical analysis with reference tissue. Parametric maps were generated using voxel-level modeling. All three compounds showed high binding potential (Bp_ND?=?k₃/k₄) in tumor voxels. [¹⁸F]AlF-NOTA-PRGD2 showed comparable Bp_ND value (3.75±0.65) with those of [¹⁸F]FPPRGD2 (3.39±0.84) and [⁶⁸Ga]Ga-NOTA-PRGD2 (3.09±0.21) (p>0.05). Little difference was found in volume of distribution (V_T) among these three RGD tracers in tumor, liver and muscle. Parametric maps showed similar kinetic parameters for all three tracers. We also demonstrated that the impact of non-specific binding could be eliminated in the kinetic analysis. Consequently, kinetic parameter estimation showed more comparable results among groups than static image analysis. In conclusion, [¹⁸F]AlF-NOTA-PRGD2 and [⁶⁸Ga]Ga-NOTA-PRGD2 have comparable pharmacokinetics and quantitative parameters compared to those of [¹⁸F]FPPRGD2. Despite the apparent difference in tumor uptake (%ID/g determined from static images) and clearance pattern, the actual specific binding component extrapolated from kinetic modeling appears to be comparable for all three dimeric RGD tracers. More...