DCFBC 

DCFBC is a prostate-specific membrane antigen (PSMA) inhibitor for small animal positron emission tomography (PET) imaging. [18F]DCFBC was prepared by reacting fluorine-18 labeled phenyl bromide with the precursor (S)-2-[3-[(R)-1-carboxy-2-thiolethyl]urea]-glutaric acid in ammonia-saturated methanol at 60°C for 10 min and then purified by C-18 reversed-phase HPLC. [18F]DCFBC was injected via the tail vein in severe combined immunodeficient mice for in vitro biodistribution or imaging. For in vitro biodistribution studies, mice were sacrificed at 5, 15, 30, 60, and 120 min after injection, and tumors, blood, and major organs were collected, weighed, and radioactivity was counted. Imaging was performed using a GE eXploreVista small animal PET scanner, collecting 12 consecutive 10-min frames. Results showed that the radiochemical yield of [18F]DCFBC averaged 16±6% (n=8) from 4-[18F]fluorophenyl bromide. Specific radioactivity ranged from 13 to 133 GBq/Amol (350-3600 Curie/mmol) with an average of 52 GBq/Amol (1392 Curie/mmol; n=6). Biodistribution and imaging studies showed high uptake of [18F]DCFBC in PIP tumors and almost no uptake in FLU tumors. High radiopharmaceutical uptake was also seen in the kidney and bladder; however, radioactivity washout from these organs was faster than from the PIP tumors. Maximum PIP tumor uptake was reached at 60 min post-injection at 8.16±2.55% injected dose/g and decreased to 4.69±0.89 at 120 min post-injection. The PIP tumor-to-muscle ratio was 20 at 120 min post-injection. Based on mouse biodistribution, the dose-limiting organ was the kidney (estimated human absorbed dose: 0.05 mGy/MBq; 0.2 rad/mCi). Conclusions: [18F]DCFBC localizes specifically to PSMA+ expressing tumors in mice and is suitable for small animal PET imaging. This novel radiopharmaceutical is an attractive candidate for further study in PET imaging of prostate cancer.

402.39

C₁₆H₁₉FN₂O₇S

564482-79-7

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