Quantitative analysis and comparison study of [18F]AlF-NOTA-PRGD2, [18F]FPPRGD2 and [68Ga]Ga-NOTA-PRGD2 using a reference tissue model.
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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DOI：
10.1371/journal.pone.0037506
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发表时间：
2012
期刊：
影响因子：
3.7
通讯作者：
Chen X
中科院分区：
文献类型：
--
作者：
Guo N;Lang L;Li W;Kiesewetter DO;Gao H;Niu G;Xie Q;Chen X
18F标记的二聚体环状α多肽([18F]β)具有良好的药代动力学和与整合素结合的亲和力，已被广泛用作正电子发射计算机断层扫描成像探针，用于病变检测和治疗反应监测。最近推出的试剂盒配方方法，使用18F-氟化铝络合物标记的RGD示踪剂([18F]Alf-NOTA-PRGD2)，提供了一种简化标记程序的策略，以促进临床翻译。同时，易于制备的68Ga标记的NOTA-PRGD2也被报道具有良好的成像整合素αvβ3的性质。本研究的目的是定量比较[18F]FPRGD2，[18F]AlF-NOTA-PRGD2和[68Ga]Ga-NOTA-PRGD2的药代动力学参数。在注射三种示踪剂后，U87 MG荷瘤小鼠接受了60分钟的动态PET扫描。以参比组织为参照物，用Logan图形分析计算动力学参数。使用体素级别建模生成参数贴图。这三个化合物在肿瘤体素中都显示出高结合势(BpND、 = 、K3/K4)。[18F]AlF-NOTA-PRGD2的BpND值(3.75±0.65)与[18F]FPPRGD2(3.39±0.84)和[68Ga]Ga-NOTA-PRGD2(3.09±0.21)相当(p>；0.05)。三种RGD示踪剂在肿瘤、肝脏和肌肉中的分布体积(VT)差异不大。参数图显示所有三种示踪剂的动力学参数相似。我们还证明了在动力学分析中可以消除非特异性结合的影响。因此，动态参数估计在组间显示出比静态图像分析更可比的结果。总之，与[18F]FPPRGD2相比，[18F]Alf-NOTA-PRGD2和[68Ga]Ga-NOTA-PRGD2具有相似的药代动力学和定量参数。尽管肿瘤摄取(从静态图像确定的%ID/g)和清除模式存在明显差异，但从动力学模型推断的实际特定结合成分似乎与所有三种二聚体RGD示踪剂相似。
With favorable pharmacokinetics and binding affinity for αvβ3 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 αvβ3. 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 (BpND = k3/k4) in tumor voxels. [18F]AlF-NOTA-PRGD2 showed comparable BpND 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 (VT) 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.
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影响因子：
12.4
作者：
Liu S;Liu H;Ren G;Kimura RH;Cochran JR;Cheng Z
通讯作者：
Cheng Z
影响因子：
3.1
作者：
Chen, XY;Liu, S;Conti, PS
通讯作者：
Conti, PS
影响因子：
9.3
作者：
Kenny, Laura M.;Coombes, R. Charles;Aboagye, Eric O.
通讯作者：
Aboagye, Eric O.
影响因子：
64.5
作者：
BROOKS, PC;MONTGOMERY, AMP;CHERESH, DA
通讯作者：
CHERESH, DA
影响因子：
4.7
作者：
Lang, Lixin;Li, Weihua;Guo, Ning;Ma, Ying;Zhu, Lei;Kiesewetter, Dale O.;Shen, Baozhong;Niu, Gang;Chen, Xiaoyuan
通讯作者：
Chen, Xiaoyuan