분자영상 및 방사화학

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  • [Biochem Biophys Res Commun .] Evaluation of PSMA target diagnostic PET tracers for therapeutic monitoring of [177Lu]ludotadipep of prostate cancer: Screening of PSMA target efficiency and biodistribution using [18F]DCFPyL and [68Ga]PSMA-11

    퓨쳐켐 / 김민환, 지대윤*

  • 출처
    Biochem Biophys Res Commun .
  • 등재일
    2023 Apr 9
  • 저널이슈번호
    651:107-113. doi: 10.1016/j.bbrc.2023.02.003.
  • 내용

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    Abstract
    We have compared the similarity of the in vivo distribution of the prostate-specific membrane antigen (PSMA)-targeted positron emission tomography (PET) imaging agents [18F]DCFPyL, [68Ga]galdotadipep, and [68Ga]PSMA-11. This study is designed for a further selection of a PSMA-targeted PET imaging agent for the therapeutic evaluation of [177Lu]ludotadipep, our previously developed prostate-specific membrane antigen (PSMA)-targeted prostate cancer therapeutic radiopharmaceutical. In vitro cell uptake was performed to evaluate the affinity to PSMA using PSMA + PC3-PIP, and PSMA- PC3-flu was used for the study. MicroPET/CT 60 min dynamic imaging and biodistribution were performed at 1, 2, and 4 h after injection. Autoradiography and immunohistochemistry were performed to evaluate the PSMA + tumor target efficiency. In the microPET/CT image, [68Ga]PSMA-11 showed the highest uptake in the kidney among all three compounds. [18F]DCFPyL and [68Ga]PSMA-11 showed similar patterns of in vivo biodistribution and high tumor targeting efficiency, similar to those of[68Ga]galdotadipep. All three agents showed high uptake in tumor tissue on autoradiography, and PSMA expression was confirmed by immunohistochemistry. Thus, [18F]DCFPyL or [68Ga]PSMA-11 can be used as a PET imaging agent to monitor [177Lu]ludotadipep therapy in prostate cancer patients.

     

     

    Affiliations

    Min Hwan Kim 1, Kyongkyu Lee 1, Keumrok Oh 1, Chul Hee Kim 1, Hee Seup Kil 1, Yong Jin Lee 2, Kyo Chul Lee 2, Dae Yoon Chi 3
    1Research Institute of Radiopharmaceuticals, FutureChem Co. Ltd, Seoul, 04793, Republic of Korea.
    2Division of Applied RI, Korea Institute of Radiological & Medical Sciences, Seoul, 01812, Republic of Korea.
    3Research Institute of Radiopharmaceuticals, FutureChem Co. Ltd, Seoul, 04793, Republic of Korea. Electronic address: daeyoon.chi@futurechem.co.kr.

  • 키워드
    MicroPET/CT; Prostate-specific membrane antigen (PSMA); [(177)Lu]Ludotadipep; [(18)F]DCFPyL; [(68)Ga]Galdotadipep; [(68)Ga]PSMA-11.
  • 편집위원

    전립선암 연구에서 prostate-specific membrane antigen (PSMA) 표적을 위한 방사성의약품의 개발은 다양하게 진행되어왔다. [177Lu]Ludotadipep은 현재 국내 임상 2상시험중에 있는 전립선암 치료용 방사성의약품인데, 이 논문은 이 치료제의 약효 모니터링을 위해 PET 영상용 제제인 [18F]DCFPyL 및 [68Ga]PSMA-11과 더불어 [177Lu]Ludotadipep 구조에 177Lu 대신 68Ga이 표지된 [68Ga]galdotadipep을 이용한 동물실험 결과를 보여주고 있다. 모두 전립선암 섭취를 잘 보여주고 있지만, 최종적으로 [18F]DCFPyL 과 [68Ga]PSMA-11이 모니터링에 가장 적합함을 보였다.

    2023-04-05 10:00:09

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