Initial clinical study of a novel prostate cancer imaging agent,&nbsp; <sup>68</sup> Ga-PSMA-4PY

ZHANG Xiaojun; LIU Huanhuan; LIU Yachao; WANG Ruimin; ZHANG Jinming

doi:10.19732/j.cnki.2096-6210.2024.04.005

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

更新时间：2025-12-15

- Initial clinical study of a novel prostate cancer imaging agent, ⁶⁸ Ga-PSMA-4PY
- Vol. 33, Issue 4, Pages: 369-375(2024)
- 作者机构：
- 作者简介：
- 基金信息：
- DOI：10.19732/j.cnki.2096-6210.2024.04.005
  CLC：
- Published Online：12 September 2024，
  
  Published：12 September 2024
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张晓军,刘欢欢,刘亚超,等. 新型前列腺癌显像剂 ⁶⁸Ga-PSMA-4PY的初步临床研究[J]. 肿瘤影像学, 2024, 33(4): 369-375 https://doi.

org/10.19732/j.cnki.2096-6210.2024.04.005
张晓军,刘欢欢,刘亚超,等. 新型前列腺癌显像剂 ⁶⁸Ga-PSMA-4PY的初步临床研究[J]. 肿瘤影像学, 2024, 33(4): 369-375 https://doi. DOI： 10.19732/j.cnki.2096-6210.2024.04.005.

org/10.19732/j.cnki.2096-6210.2024.04.005 DOI：

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

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

Ga-PSMA-4PY与

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

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，

Ga-PSMA-4PY在血液中的清除特征与

Ga-PSMA-11相近；

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

Ga-PSMA-11在肾脏中呈持续性增加，直至60 min时达到

Ga-PSMA-4PY的11倍。临床研究表明，

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

Ga-PSMA-11，且唾液腺摄取降低了57.5%。

结论：

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。

Abstract

Objective:

To evaluate the potential of

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

Ga-PSMA-4PY

nd 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

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

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

Ga-PSMA-4PY in the blood was comparable to that of

Ga-PSMA-11. The renal radiotracer uptake of

Ga-PSMA-4PY peaked within 2 min and was rapidly cleared

whereas

Ga-PSMA-11 uptake in the kidneys increased continuously

reaching 11 times higher than that of

Ga-PSMA-4PY at 60 min. Clinical studies demonstrated that

Ga-PSMA-4PY accumulated in prostate cancer lesions

with significantly lower radiotracer retention in the liver

kidneys

and spleen compared to

Ga-PSMA-11

and a reduction of 57.5% in salivary gland uptake.

Conclusion:

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.

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Related Institution

Clinical Medicine, Peking Union Medical College, Chinese Academy of Medical Sciences

Department of Nuclear Medicine, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences & Peking Union Medical College

Department of Radiotherapy, Fudan University Shanghai Cancer Center

Department of Urology, Fudan University Shanghai Cancer Center

Department of Nuclear Medicine, Fudan University Shanghai Cancer Center

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

DOI：10.19732/j.cnki.2096-6210.2024.04.005

摘要

Abstract

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