18 F-Alfatide II PET/CT in healthy human volunteers and patients with brain metastases
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We report the biodistribution and radiation dosimetry of an integrin αvβ3 specific PET tracer 18 F-AlF-NOTA-E[PEG4-c(RGDfk)]2) (denoted as 18 F-Alfatide II). We also assessed the value of 18 F-Alfatide II in patients with brain metastases.
A series of torso (from the skull to the thigh) static images were acquired in five healthy volunteers (3 M, 2 F) at 5, 10, 15, 30, 45, and 60 min after injection of 18 F-Alfatide II (257 ± 48 MBq). Regions of interest (ROIs) were drawn manually, and the time-activity curves (TACs) were obtained for major organs. Nine patients with brain metastases were examined by static PET imaging with 18 F-FDG (5.55 MBq/kg) and 18 F-Alfatide II.
Injection of 18 F-Alfatide II was well tolerated in all healthy volunteers, with no serious tracer-related adverse events found. 18 F-Alfatide II showed rapid clearance from the blood pool and kidneys. The total effective dose equivalent (EDE) and effective dose (ED) were 0.0277 ± 0.003 mSv/MBq and 0.0198 ± 0.002 mSv/MBq, respectively. The organs with the highest absorbed dose were the kidneys and the spleen. Nine patients with 20 brain metastatic lesions identified by MRI and/or CT were enrolled in this study. All 20 brain lesions were visualized by 18 F-Alfatide II PET, while only ten lesions were visualized by 18 F-FDG, and 13 by CT.
F-Alfatide II is a safe PET tracer with a favorable dosimetry profile. The observed ED suggests that 18 F-Alfatide II is feasible for human studies. 18 F-Alfatide II has potential value in finding brain metastases of different cancers as a biomarker of angiogenesis.
KeywordsRGD peptide Alfatide II Integrin PET/CT Brain metastasis
This work was supported, in part, by the National Basic Research Program of China (973 program, 2013CB733802, 2014CB744503), National Natural Science Foundation (81028009, 81171399,51473071,81472749,81401450,81471691), National Significant New Drugs Creation Program (2012ZX09505-001-001), Jiangsu Province Foundation (BE2012622, BL2012031, BM2012066,BE2014609), Outstanding Professional Fund of Health Ministry in Jiangsu Province (RC2011095,Q201406), Wuxi Social Development Project (CSZON1320), Wuxi Hospital Management Center Project (YGZXL1316), and Intramural Research Program of the National Institute of Biomedical Imaging and Bioengineering (NIBIB), National Institutes of Health (NIH).
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Statement of human rights
All procedures performed in studies involving human participants were in accordance with the ethical standards of the institutional and/or national research committee and with the 1964 Helsinki declaration and its later amendments or comparable ethical standards.
Informed consent was obtained from all individual participants included in the study.
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