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A Preliminary Study of Anti-1-Amino-3-¹⁸F-Fluorocyclobutyl-1-Carboxylic Acid for the Detection of Prostate Cancer

¹ Research Center, Nihon Medi-Physics Co., Ltd., Sodegaura, Chiba, Japan; and ² PET Center and Department of Radiology, Emory University, Atlanta, Georgia

Correspondence: For correspondence or reprints contact: Shuntaro Oka, PhD, DVM, Research Center, Nihon Medi-Physics Co., Ltd., Kitasode 3-1, Sodegaura Chiba 299-0266, Japan. E-mail: shuntaro_oka{at}nmp.co.jp

We evaluated the feasibility of anti-1-amino-3-¹⁸F-fluorocyclobutyl-1-carboxylic acid (anti-¹⁸F-FACBC) in diagnosing prostate cancer (PCa), using a rat orthotopic prostate cancer transplantation (OPCT) model. Furthermore, using in vivo experiments, we examined the potential of anti-¹⁸F-FACBC for differentiating between PCa and inflammation and between PCa and benign prostatic hyperplasia (BPH). Methods: The OPCT model was developed by transplanting DU145, a human PCa cell line, into the ventral prostate of athymic F344 rats. To develop a dual PCa and inflammation (DPCI) model, MAT-Ly-Lu-B2—a rat PCa cell line—was transplanted subcutaneously into male Copenhagen rats. Streptozotocin was injected into the hind footpad of these rats for inducing popliteal lymphadenitis. For inducing the BPH, normal F344 rats were castrated and injected subcutaneously with testosterone propionate. In biodistribution studies, the rats were injected with anti-¹⁸F-FACBC or ¹⁸F-FDG and sacrificed at 15 or 60 min after injection. We performed dynamic small-animal PET of the abdominal portion of the OPCT rats for 60 min after the injection of anti-¹⁸F-FACBC or ¹⁸F-FDG. Results: The biodistribution in the OPCT rats at 60 min after injection showed that the uptake of anti-¹⁸F-FACBC and ¹⁸F-FDG into the PCa tissue was 1.58 ± 0.40 %ID/cm³ (percentage injected dose per cm³) and 1.48 ± 0.90 %ID/cm³, respectively (P > 0.05). The accumulation of anti-¹⁸F-FACBC in the urinary bladder at 60 min after injection was 3.09 ± 1.43 %ID/cm³, whereas that of ¹⁸F-FDG was 69.31 ± 16.55 %ID/cm³ (P < 0.05). Consequently, small-animal imaging with anti-¹⁸F-FACBC facilitated the visualization of the PCa tissue of the OPCT rats with higher contrast than ¹⁸F-FDG. Furthermore, in comparison with ¹⁸F-FDG, apparently higher ratios of PCa to inflammation and PCa to BPH accumulation of anti-¹⁸F-FACBC were demonstrated in the animal models. Conclusion: FACBC PET is believed to be useful not only for the visualization of human PCa but also for differentiating between PCa and inflammation and between PCa and BHP.

Key Words: anti-¹⁸F-FACBC • ¹⁸F-FDG • prostate cancer • small-animal imaging

COPYRIGHT © 2006 by the Society of Nuclear Medicine, Inc.

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