Clinical translation of a dual integrin αvβ3 and GRPR targeting PET radiotracer 68Ga-NOTA-BBN-RGD.

This study aims to document the first-in-human application of a (68)Ga-labeled heterodimeric peptide BBN-RGD (bombesin-RGD) that targets both integrin αvβ3 and gastrin releasing peptide receptor (GRPR). We evaluated the safety and assessed the clinical diagnosis value of (68)Ga- BBN-RGD positron emission tomography (PET)/x-ray computed tomography (CT) in prostate cancer patients in comparison with (68)Ga-BBN.

Five healthy volunteers (M 4, F 1, 28-53 y) were enrolled to validate the safety of (68)Ga-BBN-RGD. Dosimetry was calculated using the OLINDA/EXM software. A total of 13 patients with prostate cancer (4 newly diagnosed and 9 post-therapy) were enrolled. All the patients underwent PET/CT scans 15-30 min after intravenous injection of 1.85 MBq (0.05 mCi) per kilogram body weight of (68)Ga-BBN-RGD, and also accepted (68)Ga-BBN PET/CT within 2 weeks for comparison.

With a mean injected dose of 107.3 ± 14.8 MBq per patient, no side effect was found during the whole procedure and 2 weeks follow-up, demonstrating the safety of (68)Ga-BBN-RGD. A patient would be exposed to a radiation dose of 2.90 mSv with an injected dose of 129.5 MBq (3.5 mCi), which is much lower than the dose limit set by the Food and Drug Administration. In 13 patients with prostate cancer diagnosed by biopsy, (68)Ga-BBN-RGD PET/CT detected 3 out of 4 primary tumors, 14 metastatic lymph nodes and 20 bone lesions with maximum standardized uptake values (SUVmax) of 4.46 ± 0.50, 6.26 ± 2.95, and 4.84 ± 1.57, respectively. Only 2/4 primary tumors, 5 lymph nodes and 12 bone lesions were positive on (68)Ga-BBN PET/CT with the SUVmax of 2.98 ± 1.24, 4.17 ± 1.89, and 3.61 ± 1.85, respectively.

This study indicates the safety and the efficiency of a new type of dual integrin αvβ3 and GRPR targeting PET radiotracer in prostate cancer diagnosis and staging.

Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 2016 Aug 04 [Epub ahead of print]

Jingjing Zhang, Gang Niu, Lixin Lang, Fang Li, Xinrong Fan, Xuefeng Yan, Shaobo Yao, Weigang Yan, Li Huo, Libo Chen, Zhiyuan Li, Zhaohui Zhu, Xiaoyuan Chen

Peking Union Medical College Hospital, China;, National Institutes of Health, United States;, NIH, United States;, Peking Union Medical College Hospital, China;, Peking Union Medical College Hospital, China;, NIH, United States;, Peking Union Medical College Hospital, China;, Peking Union Medical College Hospital, China;, Peking Union Medical College hospital, China., Peking Union Medical College hospital, China., Peking Union Medical College hospital, China., Peking Union Medical College Hospital, China;, National Institutes of Health, United States;

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