Comparison of preparation for 177Lu-labeled radiopharmaceutical and its preliminary clinical application
10.3760/cma.j.cn321828-20210201-00021
- VernacularTitle:177Lu标记的放射性药物制备方法的比较及初步临床应用
- Author:
Pengjun ZHANG
1
;
Lulu ZHANG
;
Ting BU
;
Wenyu WU
;
Fei YU
;
Lei XU
;
Zisong GUAN
;
Yuqiong CHEN
;
Jin DU
;
Feng WANG
Author Information
1. 南京医科大学附属南京医院、南京市第一医院核医学科，南京 210006
- Keywords:
Isotope labeling;
Lutetium;
Octreotide;
Prostate-specific membrane antigen
- From:
Chinese Journal of Nuclear Medicine and Molecular Imaging
2022;42(10):597-601
- CountryChina
- Language:Chinese
-
Abstract:
Objective:To investigate the preparation methods and quality control of 177Lu-labeled radiopharmaceuticals, and conduct preliminary clinical application research. Methods:177Lu-1, 4, 7, 10-tetraazacyclododecane-1, 4, 7, 10-tetraacetic acid (DOTA)- D-Phe1-Tyr3-octreotide (TOC) and 177Lu-prostate specific membrane antigen (PSMA)-I&T were labeled by manual labeling and automatic labeling, respectively. Factors such as the amount of precursor and nuclide, reaction temperature, pH value, reaction time, labeling yield and specific activity were investigated. Quality control of the products were carried out, such as clarity, pH value, sterility, bacterial endotoxin and stability in vitro. 177Lu-PSMA-I&T was applied to the treatment of prostate cancer patients, and the efficacy was evaluated by SPECT/CT imaging. Paired t test was used to analyze the data. Results:The amount of precursor and nuclide, reaction temperature, pH value and reaction time of the two methods were basically the same, both with high yield and specific activity. The yield of 177Lu-DOTA-TOC automatic labeling was significantly higher than that of manual labeling (99.2±0.4)% vs (95.3±1.5)% ( t=7.17, P<0.001), and the specific activity were (91.6±13.7) vs (89.1±13.2) GBq/μmol. The yield of 177Lu-PSMA-I&T automatic labeling was also significantly higher than that of manual labeling (99.6±0.3)% vs (95.7±1.3)% ( t=8.24, P<0.001), and the specific activity were (96.1±14.3) vs (93.2±13.8) GBq/μmol. The labeled products were colorless clear solution with pH value of 6.5-7.0. The sterility and bacterial endotoxin met the requirements. The radiochemical purity of the labeled products was more than 95% after 48 h, which showed good stability. The clinical application of 177Lu-PSMA-I&T in patients with prostate cancer showed that both primary and metastatic lesions had good uptake. Conclusions:The labeling of 177Lu radiopharmaceuticals is simple and has high yield and stability. The application of automatic labeling can simplify the process, improve the yield and reduce irradiation.
