177Lu-PSMA-I&T automated radiolabeling and preclinical prostate cancer targeting research
10.3760/cma.j.issn.2095-2848.2019.11.006
- VernacularTitle: 177Lu－PSMA－I&T的自动化合成及靶向前列腺癌的实验研究
- Author:
Lulu ZHANG
1
;
Fan QIU
1
;
Pengjun ZHANG
1
;
Zhihong XU
2
;
Ting BU
1
;
Shiming ZANG
1
;
Shuyue AI
1
;
Feng WANG
1
Author Information
1. Department of Nuclear Medicine, Nanjing First Hospital, Nanjing Medical University, Nanjing 210006, China
2. Department of Drug Research, Jiangsu Huayi Technology Co.Ltd., Changshu 215522, China
- Publication Type:Journal Article
- Keywords:
Prostatic neoplasms;
Prostate-specific membrane antigen;
Isotope labeling;
Lutetium;
Chemical synthesis;
Tumor cells, cultured;
Mice, nude
- From:
Chinese Journal of Nuclear Medicine and Molecular Imaging
2019;39(11):665-669
- CountryChina
- Language:Chinese
-
Abstract:
Objective:To synthesis 177Lu-prostate specific membrane antigen (PSMA)-I&T with automated module, evaluate the biodistribution and pharmacokinetics in mice and study the targeting property in human prostate cancer cell line LNCaP Clone FGC.
Methods:The iQS-TS automated module was applied in labeling 177Lu-PSMA-I&T. Radiochemical purity and stability were determined with high performance liquid chromatography (HPLC). The biodistribution was observed in normal ICR mice and U-SPECT/CT imaging was performed in LNCaP Clone FGC tumor-bearing mice. Independent-sample t test was used to analyze the data.
Results:177Lu-PSMA-I&T was stable in vitro and in vivo, with the radiolabeled yield of (91.5±4.9)% and radiochemical purity >99%. The half maximal inhibitory concentration (IC50) of 177Lu-PSMA-I&T binding to LNCaP Clone FGC cells was (26.74±3.53) nmol/L. The uptake of 177Lu-PSMA-I&T by LNCaP Clone FGC cells increased with time and significantly decreased after the inhibitor addition (t values: 4.301-27.483, all P<0.05). 177Lu-PSMA-I&T was cleared from blood rapidly and predominantly excreted by kidneys. Significant radioactive uptake was observed in tumors with a long retention time.
Conclusion:177Lu-PSMA-I&T can be produced in a convenient and efficient procedure using iQS-TS automated module, with good biological properties and excellent affinity and targeting property towards prostate cancer cells, which making it a potential radiopharmaceutical for prostate cancer therapy.
