新型前列腺癌显像剂68Ga-PSMA-4PY的初步临床研究
Initial clinical study of a novel prostate cancer imaging agent,68Ga-PSMA-4PY
张晓军 1刘欢欢 1刘亚超 1王瑞民 1张锦明1
作者信息
- 1. 解放军总医院第一医学中心核医学科,北京 100853
- 折叠
摘要
目的:评估一种体内快速清除的前列腺癌显像剂68Ga-PSMA-4PY在临床应用中的潜力.方法:采用前体药盒化方法标记68Ga-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68Ga-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68Ga-PSMA-4PY与68Ga-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68Ga-PSMA-4PY具有良好的标记效率和稳定性.小鼠动态PET结果显示,68Ga-PSMA-4PY在血液中的清除特征与68Ga-PSMA-11相近;68Ga-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68Ga-PSMA-11在肾脏中呈持续性增加,直至60 min时达到68Ga-PSMA-4PY的11倍.临床研究表明,68Ga-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68Ga-PSMA-11,且唾液腺摄取降低了57.5%.结论:68Ga-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.
Abstract
Objective:To evaluate the potential of 68Ga-PSMA-4PY,a prostate cancer imaging agent characterized by rapid clearance from the body,for clinical application.Methods:The precursor was kit-labeled with 68Ga-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 68Ga-PSMA-4PY in the blood,liver,and kidneys of mice.Clinical imaging studies compared the distribution characteristics of 68Ga-PSMA-4PY with those of 68Ga-PSMA-11 in prostate cancer patients.Results:The kit-labeled 68Ga-PSMA-4PY exhibited good labeling efficiency and stability.Dynamic PET imaging in mice revealed that the clearance profile of 68Ga-PSMA-4PY in the blood was comparable to that of 68Ga-PSMA-11.The renal radiotracer uptake of 68Ga-PSMA-4PY peaked within 2 min and was rapidly cleared,whereas 68Ga-PSMA-11 uptake in the kidneys increased continuously,reaching 11 times higher than that of 68Ga-PSMA-4PY at 60 min.Clinical studies demonstrated that 68Ga-PSMA-4PY accumulated in prostate cancer lesions,with significantly lower radiotracer retention in the liver,kidneys,and spleen compared to 68Ga-PSMA-11,and a reduction of 57.5%in salivary gland uptake.Conclusion:68Ga-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Key words
Prostate cancer/Positron emission tomography/computed tomography/Prostate specific membrane antigen/Clinical evaluation引用本文复制引用
出版年
2024
NETL
NSTL
万方数据