用于乳腺癌临床前PET成像的（68）Ga - AMBA和（18）F - FDG：他莫昔芬治疗对肿瘤示踪剂摄取的影响
(68)Ga-AMBA and (18)F-FDG for preclinical PET imaging of breast cancer: effect of tamoxifen treatment on tracer uptake by tumor.
作者信息
Prignon A, Nataf V, Provost C, Cagnolini A, Montravers F, Gruaz-Guyon A, Lantry L E, Talbot J N, Nunn A D
机构信息
Plateforme LIMP, UMS28 Phénotypage du petit animal, UPMC, Paris, France.
Plateforme LIMP, UMS28 Phénotypage du petit animal, UPMC, Paris, France; APHP, Hôpital Tenon, Médecine nucléaire, Paris, France.
出版信息
Nucl Med Biol. 2015 Feb;42(2):92-8. doi: 10.1016/j.nucmedbio.2014.10.003. Epub 2014 Oct 13.
INTRODUCTION
AMBA is a bombesin analogue that binds to GRPr. In a mouse model of estrogen-dependent human breast cancer, we tested whether (68)Ga-AMBA can be used for PET detection of GRPr-expressing tumors and could be more accurate than (18)F-FDG to monitor tumor response to hormone therapy.
METHODS
The radiolabeling of (68)Ga-AMBA was automated using a R&D Synchrom module. ZR75-1, a breast cancer cell line, was xenografted in nude mice. (68)Ga-AMBA tumor uptake was compared with that of (18)F-FDG before and after treatment with tamoxifen.
RESULTS
AMBA was (68)Ga-radiolabelled in 30min with 95.3% yield and purity≥98%. Prior to treatment, (68)Ga-AMBA was highly concentrated into tumors (tumor to non-tumor ratio=2.4 vs. 1.3 with (18)F-FDG). With tamoxifen treatment (n=6) (68)Ga-AMBA uptake plateaued after 1week and decreased after 2weeks, with a significant reduction compared to controls (n=4). In contrast the effect of tamoxifen treatment could not be appreciated using (18)F-FDG.
CONCLUSIONS
(68)Ga-AMBA appeared better than (18)F-FDG to visualize and monitor the response to hormone treatment in this breast cancer model.
引言
AMBA是一种与胃泌素释放肽受体（GRPr）结合的蛙皮素类似物。在雌激素依赖性人类乳腺癌小鼠模型中，我们测试了（68）Ga-AMBA是否可用于PET检测表达GRPr的肿瘤，以及在监测肿瘤对激素治疗的反应方面是否比（18）F-FDG更准确。
方法
使用研发同步模块自动进行（68）Ga-AMBA的放射性标记。将乳腺癌细胞系ZR75-1接种到裸鼠体内。比较他莫昔芬治疗前后（68）Ga-AMBA的肿瘤摄取与（18）F-FDG的肿瘤摄取情况。
结果
AMBA在30分钟内被（68）Ga放射性标记，产率为95.3%，纯度≥98%。治疗前，（68）Ga-AMBA高度浓聚于肿瘤中（肿瘤与非肿瘤比值=2.4，而（18）F-FDG为1.3）。他莫昔芬治疗（n=6）后，（68）Ga-AMBA摄取在1周后达到平台期，2周后下降，与对照组（n=4）相比有显著降低。相比之下，使用（18）F-FDG无法观察到他莫昔芬治疗的效果。
结论
在该乳腺癌模型中，（68）Ga-AMBA在可视化和监测激素治疗反应方面似乎优于（18）F-FDG。
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