Передовые методы в биологии и медицине
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ISSN: 2379-1764
ISSN: 2379-1764
Jae Cheong Lim, So Hee Dho, Eun Ha Cho, So Yo
Our previous study demonstrated the therapeutic efficacy of 177Lu-DOTA-gluBBN for the treatment of GRPRexpressing prostate tumors. As a matched pair for 177Lu, the development of labeling and molecular imaging technology using 68Ga is needed to introduce the “theranostic” approach. Therefore, the present study described the 68Ga-labeled bombesin analog, 68Ga-DOTA-gluBBN for the imaging of GRPR-expressing prostate tumors.
Methods: 68Ga was concentrated and labeled with DOTA-gluBBN using the NaCl method, and the labeling yield was evaluated by iTLC-SG. Human prostate PC-3 tumor cells were used to induce a subcutaneously xenografted-tumor model and a peritoneal metastasized tumor model. PET-CT imaging studies were performed in both animal models.
Results: Eluted 68Ga solution containing 5~10% of impurities was purified (>99%) and labeled with DOTA-gluBBN with a high incorporation yield (>98%). The total preparation time from the elution and quality control steps required below twenty minutes. 68Ga-DOTA-gluBBN was clearly visualized in xenografted PC-3 tumors at 1 hr p.i., and the tumor-tomuscle ratio was 1.7-fold higher than that observed using 18F-FDG. In a peritoneal metastasized tumor model, PC-3 tumors were widespread in peritoneum. The metastases could not be specifically visualized by PET imaging, but the tumor uptake was confirmed by ex-vivo autoradiography.
Conclusion: Favorable preclinical results demonstrating specific and effective imaging of GRPR-expressing prostate tumor recommend the further evaluation of 68Ga-DOTA-gluBBN in a clinical study to introduce a theranostic approach for prostate carcinoma patients.