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[ 18/19 F]- 4, an anionic GCPII/PSMA inhibitor for image-guided intervention in prostate cancer, is described. [ 19 F]- 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. [ 19 F]- 4 allows PSMA expression to be imaged by fluorescence (FL) and [ 18 F]-PET. PC3-PIP (PSMA-positive, EC 50 = 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 [ 18/19 F]- 4 PET, fluorescence, scintillated biodistribution, and PSMA expression are observed.
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Kommidi et al. (2018) studied this question.
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