[18/19F]-4, an anionic GCPII/PSMA inhibitor for image-guided intervention in prostate cancer, is described. [19F]-4 is radiolabeled with a radiochemical yield that is ≥27% and a molar activity of 190 ± 50 mCi/μmol in a <1 h, one-step, aqueous isotopic exchange reaction. [19F]-4 allows PSMA expression to be imaged by fluorescence (FL) and [18F]-PET. PC3-PIP (PSMA-positive, EC50 = 6.74 ± 1.33 nM) cancers are specifically delineated in mice that bear 3 million (18 mg) PC3-PIP and PC3 (control, PSMA-negative) cells. Colocalization of [18/19F]-4 PET, fluorescence, scintillated biodistribution, and PSMA expression are observed.
Journal of medicinal chemistry. 2018 Apr 20 [Epub ahead of print]
Harikrishna Kommidi, Hua Guo, Fuad Nurili, Yogindra Vedvyas, Moonsoo M Jin, Timothy D McClure, Behfar Ehdaie, Haluk B Sayman, Oguz Akin, Omer Aras, Richard Ting
Department of Radiology, Molecular Imaging Innovations Institute , Weill Cornell Medicine , New York , New York 10065 , United States., Department of Radiology , Memorial Sloan Kettering Cancer Center , New York , New York 10065 , United States., Department of Urology , Weill Cornell Medicine , New York , New York 10065 , United States., Urology Service, Department of Surgery , Memorial Sloan Kettering Cancer Center , New York , New York 10065 , United States., Department of Nuclear Medicine, Cerrahpasa Medical Faculty , Istanbul University , Fatih, Istanbul 34303 , Turkey.