新型前列腺癌显像剂^(68)Ga-PSMA-4PY的初步临床研究  

Initial clinical study of a novel prostate cancer imaging agent,^(68)Ga-PSMA-4PY

作　　者：张晓军[1] 刘欢欢[1] 刘亚超[1] 王瑞民[1] 张锦明[1] ZHANG Xiaojun;LIU Huanhuan;LIU Yachao;WANG Ruimin;ZHANG Jinming(Department of Nuclear Medicine,The First Medical Center,Chinese PLA General Hospital,Beijing 100853,China)

机构地区：[1]解放军总医院第一医学中心核医学科,北京100853

出　　处：《肿瘤影像学》2024年第4期369-375,共7页Oncoradiology

摘　　要：目的:评估一种体内快速清除的前列腺癌显像剂^(68)Ga-PSMA-4PY在临床应用中的潜力。方法:采用前体药盒化方法标记^(68)Ga-PSMA-4PY,进行质量控制确保其纯度和安全性;通过动态正电子发射体层成像(positron emission tomography,PET)分析^(68)Ga-PSMA-4PY在小鼠血液、肝脏和肾脏中的放射性摄取及清除。并通过临床显像研究比较^(68)Ga-PSMA-4PY与^(68)Ga-PSMA-11在前列腺癌患者体内的分布特性。结果:经前体药盒化标记的^(68)Ga-PSMA-4PY具有良好的标记效率和稳定性。小鼠动态PET结果显示,^(68)Ga-PSMA-4PY在血液中的清除特征与^(68)Ga-PSMA-11相近;^(68)Ga-PSMA-4PY在肾脏中的放射性摄取峰值出现在2 min内,并随后快速排出,而^(68)Ga-PSMA-11在肾脏中呈持续性增加,直至60 min时达到^(68)Ga-PSMA-4PY的11倍。临床研究表明,^(68)Ga-PSMA-4PY可以在前列腺癌中浓集,在肝、肾和脾脏中的放射性滞留明显低于^(68)Ga-PSMA-11,且唾液腺摄取降低了57.5%。结论:^(68)Ga-PSMA-4PY能够快速浓聚到PSMA阳性的肿瘤中,并迅速从正常组织中清除,将有助于减少非特异性摄取引起的不良反应,是一种具有良好前景的前列腺癌显像剂。Objective:To evaluate the potential of^(68)Ga-PSMA-4PY,a prostate cancer imaging agent characterized by rapid clearance from the body,for clinical application.Methods:The precursor was kit-labeled with^(68)Ga-PSMA-4PY,and quality control measures ensured its purity and safety.Dynamic positron emission tomography(PET)imaging was used to study the radiotracer uptake and clearance dynamics of^(68)Ga-PSMA-4PY in the blood,liver,and kidneys of mice.Clinical imaging studies compared the distribution characteristics of^(68)Ga-PSMA-4PY with those of^(68)Ga-PSMA-11 in prostate cancer patients.Results:The kit-labeled^(68)Ga-PSMA-4PY exhibited good labeling efficiency and stability.Dynamic PET imaging in mice revealed that the clearance profileof^(68)Ga-PSMA-4PY in the blood was comparable to that of^(68)Ga-PSMA-11.The renal radiotracer uptake of^(68)Ga-PSMA-4PY peaked within 2 min and was rapidly cleared,whereas^(68)Ga-PSMA-11 uptake in the kidneys increased continuously,reaching 11 times higher than that of^(68)Ga-PSMA-4PY at 60 min.Clinical studies demonstrated that^(68)Ga-PSMA-4PY accumulated in prostate cancer lesions,with significantly lower radiotracer retention in the liver,kidneys,and spleen compared to^(68)Ga-PSMA-11,and a reduction of 57.5%in salivary gland uptake.Conclusion:^(68)Ga-PSMA-4PY can rapidly accumulate in PSMA-positive tumors and clear quickly from normal tissues,which will help reduce nonspecific uptake and associated side effects,making it a promising prostate cancer imaging agent.

关 键 词：前列腺癌 正电子发射体层成像/计算机体层成像 前列腺特异性膜抗原 临床评价 

分 类 号：R737.25[医药卫生—肿瘤] R445.5[医药卫生—临床医学]