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OtherBasic Science (Animal or Phantoms)
Open Access

68Ga-DOTA-NT-20.3 Neurotensin receptor 1 positron emission tomography imaging as a surrogate for neuroendocrine differentiation of prostate cancer

Wen Yu Wu, Fei Yu, Peng Jun Zhang, Ting Bu, Jing Jing Fu, Shu Yue Ai, Qin Qin You, Liang Shi, Guo Qiang Shao, Feng Wang, Marina Hodolic and Hong Qian Guo
Journal of Nuclear Medicine February 2022, jnumed.121.263132; DOI: https://doi.org/10.2967/jnumed.121.263132
Wen Yu Wu
1 Department of Nuclear Medicine, Nanjing First Hospital, Nanjing Medical University, China;
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Fei Yu
1 Department of Nuclear Medicine, Nanjing First Hospital, Nanjing Medical University, China;
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Peng Jun Zhang
1 Department of Nuclear Medicine, Nanjing First Hospital, Nanjing Medical University, China;
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Ting Bu
1 Department of Nuclear Medicine, Nanjing First Hospital, Nanjing Medical University, China;
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Jing Jing Fu
1 Department of Nuclear Medicine, Nanjing First Hospital, Nanjing Medical University, China;
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Shu Yue Ai
1 Department of Nuclear Medicine, Nanjing First Hospital, Nanjing Medical University, China;
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Qin Qin You
1 Department of Nuclear Medicine, Nanjing First Hospital, Nanjing Medical University, China;
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Liang Shi
1 Department of Nuclear Medicine, Nanjing First Hospital, Nanjing Medical University, China;
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Guo Qiang Shao
1 Department of Nuclear Medicine, Nanjing First Hospital, Nanjing Medical University, China;
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Feng Wang
1 Department of Nuclear Medicine, Nanjing First Hospital, Nanjing Medical University, China;
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Marina Hodolic
2 Nuclear Medicine Research Department, IASON, Graz, Austria;
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Hong Qian Guo
3 Department of Urology, Drum Tower Hospital, Medical School of Nanjing University, China
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Abstract

PSMA-negative neuroendocrine prostate cancer (NEPC) is likely to be a lethal subtype of prostate cancer (PCa) with limited clinical diagnostic and therapeutic options. High expression of neurotensin receptor subtype 1 (NTR1) associated with neuroendocrine differentiation of PCa, which makes NTR1 a potential target for NEPC. In this study, NTR1-targeted tracer 68Ga-DOTA-NT-20.3 was synthesized and evaluated by determining its affinity to androgen-dependent (LNCap) and androgen-independent (PC3) xenografts. Methods: 68Ga-DOTA-NT-20.3 was labeled with an automated iQS-theranostics synthesizer module and its stability, labeling yield, and radiochemical purity were analyzed by radio-HPLC. Receptor binding affinity was evaluated in NTR1-positive PC3 cells by competitive binding assay. The biodistribution of 68Ga-DOTA-NT-20.3 in vivo was evaluated in PC3 and LNCap xenografts by micro-PET imaging. NTR1 expression was identified by immunohistochemistry and immunofluorescence. Results: 68Ga-DOTA-NT-20.3 was synthesized successfully with a yield rate of 88.07 ± 1.26 %, radiochemical purity ≥ 99% and favorable stability. The NTR1 affinity (IC50) for 68Ga-DOTA-NT-20.3 was 7.59 ± 0.41 nM. Micro-PET/CT in PC3 xenografts showed high contrast images with intense tumor uptake, which revealed specific NTR1 expression. The tumor showed significant radioactivity (4.95 ± 0.67 percentage of injected dose per gram of tissue [%ID/g]) at 1h, which fell to 1.95 ± 0.17 %ID/g (P < 0.01, t = 8.72) after specific blockage by neurotensin. LNCap xenografts had no significant accumulation (0.81 ± 0.06 %ID/g) of 68Ga-DOTA-NT-20.3 at 1 h. In contrast, 68Ga-PSMA-11 was mainly concentrated in LNCap xenografts (8.60 ± 2.11 %ID/g), with no significant uptake in PC3 tumors (0.53 ± 0.05 %ID/g), consistent with the in vitro immunohistochemistry findings. Biodistribution showed rapid clearance from the blood and main organs (brain, heart, lung, liver, muscle, bone) with significantly high tumor/liver (4.41 ± 0.73) and tumor/muscle ratios (12.34 ± 1.32) at 60 min post-injection. Conclusion: 68Ga-DOTA-NT-20.3 can be efficiently prepared with a high yield and radiochemical purity. Its favorable biodistribution and prominent NTR1 affinity make 68Ga-DOTA-NT-20.3 a potential radiopharmaceutical for the detection of PSMA-negative PCa and identification of neuroendocrine differentiation.

  • Genitourinary
  • Molecular Imaging
  • Peptides
  • PET/CT
  • 68Ga-DOTA-NT-20.3
  • PET
  • neuroendocrine differentiation
  • neurotensin receptor subtype 1
  • prostate cancer

Footnotes

  • Immediate Open Access: Creative Commons Attribution 4.0 International License (CC BY) allows users to share and adapt with attribution, excluding materials credited to previous publications. License: https://creativecommons.org/licenses/by/4.0/. Details: https://jnm.snmjournals.org/page/permissions.

  • Copyright © 2022 by the Society of Nuclear Medicine and Molecular Imaging, Inc.

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Journal of Nuclear Medicine
Vol. 63, Issue 5
May 1, 2022
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68Ga-DOTA-NT-20.3 Neurotensin receptor 1 positron emission tomography imaging as a surrogate for neuroendocrine differentiation of prostate cancer
Wen Yu Wu, Fei Yu, Peng Jun Zhang, Ting Bu, Jing Jing Fu, Shu Yue Ai, Qin Qin You, Liang Shi, Guo Qiang Shao, Feng Wang, Marina Hodolic, Hong Qian Guo
Journal of Nuclear Medicine Feb 2022, jnumed.121.263132; DOI: 10.2967/jnumed.121.263132

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68Ga-DOTA-NT-20.3 Neurotensin receptor 1 positron emission tomography imaging as a surrogate for neuroendocrine differentiation of prostate cancer
Wen Yu Wu, Fei Yu, Peng Jun Zhang, Ting Bu, Jing Jing Fu, Shu Yue Ai, Qin Qin You, Liang Shi, Guo Qiang Shao, Feng Wang, Marina Hodolic, Hong Qian Guo
Journal of Nuclear Medicine Feb 2022, jnumed.121.263132; DOI: 10.2967/jnumed.121.263132
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Keywords

  • Genitourinary
  • molecular imaging
  • Peptides
  • PET/CT
  • 68Ga-DOTA-NT-20.3
  • PET
  • neuroendocrine differentiation
  • neurotensin receptor subtype 1
  • prostate cancer
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