Abstract | PURPOSE: The chemokine receptor CXCR4 is overexpressed in various types of human cancers. As a specific imaging agent of CXCR4, (68)Ga-NOTA-NFB was investigated in this study to assess its safety, biodistribution and dosimetry properties in healthy volunteers, and to preliminarily evaluate its application in glioma patients. METHODS: Six healthy volunteers underwent whole-body PET scans at 0, 0.5, 1, 2 and 3 h after (68)Ga-NOTA-NFB injection (mean dose, 182.4 ± 3.7 MBq (4.93 ± 0.10 mCi)). For time-activity curve calculations, 1 mL blood samples were obtained at 1, 3, 5, 10, 30, 60, 90, 120, 150 and 180 min after the injection. The estimated radiation doses were calculated by OLINDA/EXM software. Eight patients with glioma were enrolled and underwent both (68)Ga-NOTA-NFB and (18)F-FDG PET/CT scans before surgery. The expression of CXCR4 on the resected brain tumor tissues was determined by immunohistochemical staining. RESULTS: (68)Ga-NOTA-NFB was safe and well tolerated by all subjects. A rapid activity clearance from the blood circulation was observed. The organs with the highest absorbed doses were spleen (193.8 ± 32.5 μSv/MBq) and liver (119.3 ± 25.0 μSv/MBq). The mean effective dose was 25.4 ± 6.1 μSv/MBq. The maximum standardized uptake values (SUVmax) and the maximum target to non-target ratios (T/NTmax) of (68)Ga-NOTA-NFB PET/CT in glioma tissues were 4.11 ± 2.90 (range, 0.45-8.21) and 9.21 ± 8.75 (range, 3.66-24.88), respectively, while those of (18)F-FDG PET/CT were 7.34 ± 2.90 (range, 3.50-12.27) and 0.86 ± 0.41 (range, 0.35-1.59). The histopathological staining confirmed that CXCR4 was overexpressed on resected tumor tissues with prominent (68)Ga-NOTA-NFB uptake. CONCLUSION: With a favorable radiation dosimetry profile, (68)Ga-NOTA-NFB is safe for clinical imaging. Compared to (18)F-FDG PET/CT, (68)Ga-NOTA-NFB PET/CT is more sensitive in detecting glioma and could have potential in diagnosing and treatment planning for CXCR4 positive patients.
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Authors | Zhe Wang, Mingru Zhang, Liang Wang, Shengjun Wang, Fei Kang, Guoquan Li, Orit Jacobson, Gang Niu, Weidong Yang, Jing Wang, Xiaoyuan Chen |
Journal | Theranostics
(Theranostics)
Vol. 5
Issue 8
Pg. 882-9
( 2015)
ISSN: 1838-7640 [Electronic] Australia |
PMID | 26000059
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- CXCR4 protein, human
- Gallium Radioisotopes
- Receptors, CXCR4
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Topics |
- Adult
- Aged
- Female
- Gallium Radioisotopes
(administration & dosage)
- Glioma
(diagnosis)
- Healthy Volunteers
- Humans
- Male
- Middle Aged
- Positron-Emission Tomography
(methods)
- Prospective Studies
- Radiometry
(methods)
- Receptors, CXCR4
(analysis)
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