title: (68)Ga-labeled 3PRGD2 for dual PET and Cerenkov luminescence imaging of orthotopic human glioblastoma.
abstract: β-Emitters can produce Cerenkov radiation that is detectable by Cerenkov luminescence imaging (CLI), allowing the combination of PET and CLI with one radiotracer for both tumor diagnosis and visual guidance during surgery. Recently, the clinical feasibility of CLI with the established therapeutic reagent Na(131)I and the PET tracer (18)F-FDG was demonstrated. (68)Ga possesses a higher Cerenkov light output than (18)F and (131)I, which would result in higher sensitivity for CLI and improve the outcome of CLI in clinical applications. However, the research on (68)Ga-based tumor-specific tracers for CLI is limited. In this study, we examined the use of (68)Ga-radiolabeled DOTA-3PRGD2 ((68)Ga-3PRGD2) for dual PET and CLI of orthotopic U87MG human glioblastoma. For this purpose, the Cerenkov efficiencies of (68)Ga and (18)F were measured with the IVIS Spectrum system (PerkinElmer, USA). The CLI signal intensity of (68)Ga was 15 times stronger than that of (18)F. PET and CLI of (68)Ga-3PRGD2 were performed in U87MG human glioblastoma xenografts. Both PET and CLI revealed a remarkable accumulation of (68)Ga-3PRGD2 in the U87MG human glioblastoma xenografts at 1 h p.i. with an extremely low background in the brain when compared with (18)F-FDG. Furthermore, (68)Ga-3PRGD2 was used for dual PET and CLI of orthotopic human glioblastoma. The orthotopic human glioblastoma was clearly visualized by both imaging modalities. In addition, the biodistribution of (68)Ga-3PRGD2 was assessed in normal mice to estimate the radiation dosimetry. The whole-body effective dose is 20.1 ± 3.3 μSv/MBq, which is equal to 3.7 mSv per whole-body PET scan with a 5 mCi injection dose. Thus, (68)Ga-3PRGD2 involves less radiation exposure in patients when compared with (18)F-FDG (7.0 mSv). The use of (68)Ga-3PRGD2 in dual PET and CLI shows great promise for tumor diagnosis and image-guided surgery.
authors: Di
authors: D
authors: Fan
authors: Xin
authors: X
authors: Zhang
authors: Lijun
authors: L
authors: Zhong
authors: Xujie
authors: X
authors: Liu
authors: §Department of Nuclear Medicine, Peking Union Medical College Hospital, Beijing 100857, China.
authors: Yi
authors: Y
authors: Sun
authors: Huiyun
authors: H
authors: Zhao
authors: Bing
authors: B
authors: Jia
authors: Zhaofei
authors: Z
authors: Liu
authors: §Department of Nuclear Medicine, Peking Union Medical College Hospital, Beijing 100857, China.
authors: Zhaohui
authors: Z
authors: Zhu
authors: ∥Interdisciplinary Laboratory, Institute of Biophysics, Chinese Academy of Sciences, Beijing 100101, China.
authors: Jiyun
authors: J
authors: Shi
authors: ∥Interdisciplinary Laboratory, Institute of Biophysics, Chinese Academy of Sciences, Beijing 100101, China.
authors: Fan
authors: F
authors: Wang
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D005260:Female; D019788:Fluorodeoxyglucose F18 / Q000493:pharmacokinetics; D005710:Gallium Radioisotopes / Q000737:chemistry* / Q000493:pharmacokinetics; D005909:Glioblastoma / Q000175:diagnosis*; D006801:Humans; D049449:Luminescence; D008163:Luminescent Measurements / Q000379:methods; D051379:Mice; D008807:Mice, Inbred BALB C; D009842:Oligopeptides / Q000737:chemistry* / Q000493:pharmacokinetics; D061848:Optical Imaging / Q000379:methods*; D009942:Organometallic Compounds / Q000737:chemistry* / Q000493:pharmacokinetics; D010456:Peptides, Cyclic / Q000737:chemistry* / Q000493:pharmacokinetics; D049268:Positron-Emission Tomography / Q000379:methods*; D014018:Tissue Distribution
chemical_list: C532505:68Ga-DOTA-cyclo(arginyl-glycyl-aspartyl-phenylalanyl-lysyl); D005710:Gallium Radioisotopes; D009842:Oligopeptides; D009942:Organometallic Compounds; D010456:Peptides, Cyclic; D019788:Fluorodeoxyglucose F18; C047981:arginyl-glycyl-aspartic acid