title: First experience of 18F-alfatide in lung cancer patients using a new lyophilized kit for rapid radiofluorination.
abstract: (18)F-FPPRGD2, which was approved for clinical study recently, has favorable properties for integrin targeting and showed potential for antiangiogenic therapy and early response monitoring. However, the time-consuming multiple-step synthesis may limit its widespread applications in the clinic. In this study, we developed a simple lyophilized kit for labeling PRGD2 peptide ((18)F-AlF-NOTA-PRGD2, denoted as (18)F-alfatide) using a fluoride-aluminum complex that significantly simplified the labeling procedure.
  
  
  METHODS
  Nine patients with a primary diagnosis of lung cancer were examined by both static and dynamic PET imaging with (18)F-alfatide, and 1 tuberculosis patient was investigated using both (18)F-alfatide and (18)F-FDG imaging. Standardized uptake values were measured in tumors and other main organs at 30 min and 1 h after injection. Kinetic parameters were calculated by Logan graphical analysis. Immunohistochemistry and staining intensity quantification were performed to confirm the expression of integrin α(v)β(3).
  
  
  RESULTS
  Under the optimal conditions, the whole radiosynthesis including purification was accomplished within 20 min with a decay-corrected yield of 42.1% ± 2.0% and radiochemical purity of more than 95%. (18)F-alfatide PET imaging identified all tumors, with mean standardized uptake values of 2.90 ± 0.10. Tumor-to-muscle and tumor-to-blood ratios were 5.87 ± 2.02 and 2.71 ± 0.92, respectively.
  
  
  CONCLUSIONS
  (18)F-alfatide can be produced with excellent radiochemical yield and purity via a simple, 1-step, lyophilized kit. PET scanning with (18)F-alfatide allows specific imaging of αvβ3 expression with good contrast in lung cancer patients. This technique might be used for the assessment of angiogenesis and for planning and response evaluation of cancer therapies that would affect angiogenesis status and integrin expression levels.
authors.affiliation: Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi, China.
authors.forename: Weixing
authors.initials: W
authors.lastname: Wan
authors.forename: Ning
authors.initials: N
authors.lastname: Guo
authors.forename: Donghui
authors.initials: D
authors.lastname: Pan
authors.forename: Chunjing
authors.initials: C
authors.lastname: Yu
authors.forename: Yuan
authors.initials: Y
authors.lastname: Weng
authors.forename: Shineng
authors.initials: S
authors.lastname: Luo
authors.forename: Hong
authors.initials: H
authors.lastname: Ding
authors.forename: Yuping
authors.initials: Y
authors.lastname: Xu
authors.forename: Lizhen
authors.initials: L
authors.lastname: Wang
authors.forename: Lixin
authors.initials: L
authors.lastname: Lang
authors.forename: Qingguo
authors.initials: Q
authors.lastname: Xie
authors.forename: Min
authors.initials: M
authors.lastname: Yang
authors.forename: Xiaoyuan
authors.initials: X
authors.lastname: Chen
mesh_terms: D000368:Aged; D019281:Dimerization; D005240:Feasibility Studies; D005462:Fluorine Radioisotopes; D005612:Freeze Drying; D006801:Humans; D007553:Isotope Labeling / Q000379:methods*; D007700:Kinetics; D008175:Lung Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism; D008297:Male; D008875:Middle Aged; D018307:Neoplasms, Squamous Cell / Q000000981:diagnostic imaging / Q000378:metabolism; D009842:Oligopeptides / Q000737:chemistry / Q000493:pharmacokinetics; D049268:Positron-Emission Tomography; D012680:Sensitivity and Specificity
chemical_list: D005462:Fluorine Radioisotopes; D009842:Oligopeptides; C047981:arginyl-glycyl-aspartic acid
keywords: PET; RGD peptide; alfatide; aluminum fluoride; lung cancer
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