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Small Molecule, Multimodal, [18F]-PET and Fluorescence Imaging Agent Targeting Prostate-Specific Membrane Antigen: First-in-Human Study
Small Molecule, Multimodal, [18F]-PET and Fluorescence Imaging Agent Targeting Prostate-Specific Membrane Antigen: First-in-Human Study
- Source :
- Clin Genitourin Cancer
- Publication Year :
- 2021
- Publisher :
- Elsevier BV, 2021.
-
Abstract
- Background A first-in-human study of [18F]-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 [18F]-BF3-Cy3-ACUPA and underwent PET/computed tomography (CT) imaging. Radiation dosimetry of [18F]-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 [18F]-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. [18F]-BF3-Cy3-ACUPA physiologic radiotracer accumulation and urinary/biliary excretion closely resembled the distribution of other published PSMA tracers including [18F]-JK-PSMA-7, [18F]-PSMA-1007, [18F]-DCFPyL, and [18F]-DCFBC. 19F-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 [18F]-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.
- Subjects :
- Glutamate Carboxypeptidase II
Male
medicine.medical_specialty
Fluorescence-lifetime imaging microscopy
Biodistribution
Urology
030232 urology & nephrology
Article
03 medical and health sciences
Prostate cancer
0302 clinical medicine
Prostate
Positron Emission Tomography Computed Tomography
medicine
Humans
Tissue Distribution
medicine.diagnostic_test
business.industry
Optical Imaging
Prostatic Neoplasms
Cancer
medicine.disease
Imaging agent
medicine.anatomical_structure
Oncology
Positron emission tomography
Positron-Emission Tomography
030220 oncology & carcinogenesis
Antigens, Surface
Histopathology
Radiopharmaceuticals
business
Nuclear medicine
Subjects
Details
- ISSN :
- 15587673
- Volume :
- 19
- Database :
- OpenAIRE
- Journal :
- Clinical Genitourinary Cancer
- Accession number :
- edsair.doi.dedup.....140531ca205064d29c6115d82e174020
- Full Text :
- https://doi.org/10.1016/j.clgc.2021.03.011