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Abstract
The aim of this work was to evaluate Gd-FC705, a prostate-specific membrane antigen (PSMA)-targeted MRI contrast agent. The r1 and r2 relaxivities of Gd-FC705 are 5.94 mM-1s-1 and 17.77 mM-1s-1, respectively, in HSA solution (0.67 mM) at 3 T, which are higher than those of Gd-DOTA. Specific targeting efficacy was found with a 3-fold enhancement between PSMA-negative (PSMA-) and PSMA-positive (PSMA+) cells. The in vivo targeting and bio-distribution of Gd-FC705 were further confirmed using nude mice bearing PC3 human prostate cancer xenografts, which showed a 2-fold increase in the contrast-to-noise ratio (CNR) for PSMA+ tumors compared to PSMA- tumors 1 h post injection and a longer circulation time than Gd-DOTA. These results demonstrate that Gd-FC705 has great potential as a diagnostic agent for prostate cancer.

Affiliations

Ji-Ung Yang  1 , Soyeon Kim  2 , Jae Hun Ahn  3 , Min Hwan Kim  4 , Hee Seup Kil  4 , Dae Yoon Chi  4 , Kyo Chul Lee  2 , Yong Jin Lee  2 , Ji-Ae Park  5
1 Division of Applied RI, Korea Institute of Radiological & Medical Sciences (KIRAMS), Seoul, 01812, South Korea; Department of Medical & Biological Engineering, Kyungpook National University, Daegu, 41566, South Korea.
2 Division of Applied RI, Korea Institute of Radiological & Medical Sciences (KIRAMS), Seoul, 01812, South Korea.
3 Division of Applied RI, Korea Institute of Radiological & Medical Sciences (KIRAMS), Seoul, 01812, South Korea; Graduate School of Translational Medicine, Seoul National University College of Medicine, Seoul, 03080, South Korea.
4 Research Institute of Labeling, FutureChem Co., Ltd., Seoul, 04794, South Korea.
5 Division of Applied RI, Korea Institute of Radiological & Medical Sciences (KIRAMS), Seoul, 01812, South Korea. Electronic address: jpark@kirams.re.kr.