文献检索文档翻译深度研究
Suppr Zotero 插件Zotero 插件
邀请有礼套餐&价格历史记录

新学期，新优惠

限时优惠:9月1日-9月22日

30天高级会员仅需29元

1天体验卡首发特惠仅需5.99元

了解详情
不再提醒
插件&应用
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
高级版
套餐订阅购买积分包
AI 工具
文献检索文档翻译深度研究
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2025

小分子、多模式、[F]-PET 和荧光成像剂靶向前列腺特异性膜抗原：首例人体研究。

Small Molecule, Multimodal, [F]-PET and Fluorescence Imaging Agent Targeting Prostate-Specific Membrane Antigen: First-in-Human Study.

机构信息

Department of Radiology, Memorial Sloan Kettering Cancer Center, New York, NY, USA.

Department of Urology, Istanbul University-Cerrahpasa, Cerrahpasa Medical Faculty, Istanbul, Turkey.

出版信息

Clin Genitourin Cancer. 2021 Oct;19(5):405-416. doi: 10.1016/j.clgc.2021.03.011. Epub 2021 Mar 19.

DOI:10.1016/j.clgc.2021.03.011
PMID:33879400
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8449790/
Abstract

BACKGROUND: A first-in-human study of [F]-BF3-Cy3-ACUPA, a small-molecule imaging agent that can be unimolecularly both positron emitting and fluorescent, is conducted to determine its safety, biodistribution, radiation dosimetry, feasibility in tumor detection by preoperative positron emission tomography (PET), as well as its intraoperative fluorescence imaging utility in patients with prostate-specific membrane antigen positive (PSMA) tumors. METHODS: Ten patients aged 66 ± 7 years received a 6.5 ± 3.2 mCi intravenous injection of [F]-BF3-Cy3-ACUPA and underwent PET/computed tomography (CT) imaging. Radiation dosimetry of [F]-BF3-Cy3-ACUPA, normal organ biodistribution, and tumor uptakes were examined. Two patients were prescheduled for radical prostatectomy (RP) with extended pelvic lymphadenectomy approximately 24 hours following [F]-BF3-Cy3-ACUPA injection and imaging. Without reinjection, intraoperative fluorescence imaging was performed on freshly excised tissue during RP. Frozen sections of excised tissue during RP were submitted for confirmatory histopathology and multiphoton fluorescence and brightfield microscopy. RESULTS: Absorbed doses by organs including the kidneys and salivary glands were similar to 68Ga-PSMA-11 imaging. [F]-BF3-Cy3-ACUPA physiologic radiotracer accumulation and urinary/biliary excretion closely resembled the distribution of other published PSMA tracers including [F]-JK-PSMA-7, [F]-PSMA-1007, [F]-DCFPyL, and [F]-DCFBC. F-BF3-Cy3-ACUPA was retained in PSMA cancer tissues in patients for at least 24 hours, allowing for intraoperative fluorescence assessment of the prostate and of the embedded prostate cancer without contrast reinjection. After 24 hours, the imaging agent mostly decayed or cleared from the blood pool. Preoperative PET and fluorescence imaging findings were confirmed with final histopathology and multiphoton microscopy. CONCLUSION: Our first-in-human results demonstrate that [F]-BF3-Cy3-ACUPA is safe and feasible in humans. Larger trials with this PET tracer are expected to further define its capabilities and its clinical role in the management of PSMA tumors, especially in prostate cancer.

摘要

背景：本研究进行了一种名为 [F]-BF3-Cy3-ACUPA 的小分子成像剂的首次人体研究，该成像剂可以单分子同时发射正电子和荧光，以确定其安全性、生物分布、辐射剂量测定、术前正电子发射断层扫描（PET）检测肿瘤的可行性，以及在前列腺特异性膜抗原阳性（PSMA）肿瘤患者中的术中荧光成像应用。

方法：10 名年龄 66±7 岁的患者接受了 6.5±3.2mCi 的静脉注射 [F]-BF3-Cy3-ACUPA，并进行了 PET/CT 成像。检查了 [F]-BF3-Cy3-ACUPA 的辐射剂量测定、正常器官生物分布和肿瘤摄取情况。两名患者计划在注射 [F]-BF3-Cy3-ACUPA 并进行成像后约 24 小时进行根治性前列腺切除术（RP）和扩大盆腔淋巴结切除术。无需再次注射，在 RP 期间对刚切除的组织进行术中荧光成像。RP 期间切除组织的冷冻切片用于确认组织病理学和多光子荧光和明场显微镜。

结果：包括肾脏和唾液腺在内的器官的吸收剂量与 68Ga-PSMA-11 成像相似。[F]-BF3-Cy3-ACUPA 的生理放射性示踪剂积累和尿液/胆汁排泄与其他已发表的 PSMA 示踪剂（包括[F]-JK-PSMA-7、[F]-PSMA-1007、[F]-DCFPyL 和[F]-DCFBC）的分布非常相似。在患者中，F-BF3-Cy3-ACUPA 在至少 24 小时内保留在 PSMA 癌组织中，允许在没有对比剂再注射的情况下进行前列腺和嵌入前列腺癌的术中荧光评估。24 小时后，造影剂大部分从血池中衰变或清除。术前 PET 和荧光成像结果与最终组织病理学和多光子显微镜检查结果一致。

结论：我们的首次人体研究结果表明，[F]-BF3-Cy3-ACUPA 在人体中是安全可行的。预计更大规模的试验将进一步确定该 PET 示踪剂的能力及其在 PSMA 肿瘤管理中的临床作用，特别是在前列腺癌中。

相似文献

[1]
Small Molecule, Multimodal, [F]-PET and Fluorescence Imaging Agent Targeting Prostate-Specific Membrane Antigen: First-in-Human Study.

Clin Genitourin Cancer. 2021-10

[2]
F-18 labelled PSMA-1007: biodistribution, radiation dosimetry and histopathological validation of tumor lesions in prostate cancer patients.

Eur J Nucl Med Mol Imaging. 2017-4

[3]
A Fluorescent, [F]-Positron-Emitting Agent for Imaging Prostate-Specific Membrane Antigen Allows Genetic Reporting in Adoptively Transferred, Genetically Modified Cells.

ACS Chem Biol. 2019-6-17

[4]
Radiopharmaceutical for detecting PSMA - positive metastatic colon cancer: Matched-pair comparison of 18F-BF3-Cy3-ACUPA and 68Ga-PSMA PET/MRI.

Nucl Med Rev Cent East Eur. 2022

[5]
More advantages in detecting bone and soft tissue metastases from prostate cancer using F-PSMA PET/CT.

Hell J Nucl Med. 2019

[6]
An F-Labeled PSMA Ligand for PET/CT of Prostate Cancer: First-in-Humans Observational Study and Clinical Experience with F-JK-PSMA-7 During the First Year of Application.

J Nucl Med. 2019-7-19

[7]
Phase I Study of CTT1057, an F-Labeled Imaging Agent with Phosphoramidate Core Targeting Prostate-Specific Membrane Antigen in Prostate Cancer.

J Nucl Med. 2018-11-21

[8]
[Ga]Ga-P16-093 as a PSMA-Targeted PET Radiopharmaceutical for Detection of Cancer: Initial Evaluation and Comparison with [Ga]Ga-PSMA-11 in Prostate Cancer Patients Presenting with Biochemical Recurrence.

Mol Imaging Biol. 2020-6

[9]
Ga-Labeled Prostate-specific Membrane Antigen Ligand Positron Emission Tomography/Computed Tomography for Prostate Cancer: A Systematic Review and Meta-analysis.

Eur Urol Focus. 2016-11-15

[10]
Initial Evaluation of [(18)F]DCFPyL for Prostate-Specific Membrane Antigen (PSMA)-Targeted PET Imaging of Prostate Cancer.

Mol Imaging Biol. 2015-8

引用本文的文献

[1]
Molecular-Targeted Fluorescence Lymph Node Imaging Could Play a Clinical Role in the Surgical Setting: A Systematic Review.

Cancers (Basel). 2025-4-17

[2]
Dual-Labeled Small Peptides in Cancer Imaging and Fluorescence-Guided Surgery: Progress and Future Perspectives.

Pharmaceuticals (Basel). 2025-1-22

[3]
Lessons learned in application driven imaging agent design for image-guided surgery.

Eur J Nucl Med Mol Imaging. 2024-8

[4]
Prostate-specific membrane antigen-targeted surgery in prostate cancer: Accurate identification, real-time diagnosis, and precise resection.

Theranostics. 2024

[5]
Delphi consensus project on prostate-specific membrane antigen (PSMA)-targeted surgery-outcomes from an international multidisciplinary panel.

Eur J Nucl Med Mol Imaging. 2024-8

[6]
A novel PSMA targeted dual-function near-infrared fluorescence and PET probe for the image-guided surgery and detection of prostate cancer.

Eur J Nucl Med Mol Imaging. 2024-8

[7]
State of the Art in Prostate-specific Membrane Antigen-targeted Surgery-A Systematic Review.

Eur Urol Open Sci. 2023-6-16

[8]
Clickable -Glycosyl Scaffold for the Development of a Dual Fluorescent and [F]fluorinated Cyanine-Containing Probe and Preliminary In Vitro/Vivo Evaluation by Fluorescence Imaging.

Pharmaceuticals (Basel). 2022-11-29

[9]
Targeted Dual-Modal PET/SPECT-NIR Imaging: From Building Blocks and Construction Strategies to Applications.

Cancers (Basel). 2022-3-23

[10]
Dual Probes for Positron Emission Tomography (PET) and Fluorescence Imaging (FI) of Cancer.

Pharmaceutics. 2022-3-15

文献AI研究员

20分钟写一篇综述，助力文献阅读效率提升50倍

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

推荐工具

医学文档翻译智能文献检索