64Cu-PSMA-BCH: a new radiotracer for delayed PET imaging of prostate cancer

Teli Liu, Chen Liu, Zhongyi Zhang, Ning Zhang, Xiaoyi Guo, Lei Xia, Jinquan Jiang, Qing Xie, Kun Yan, Steven P. Rowe, Hua Zhu, Zhi Yang

Research output: Contribution to journalArticlepeer-review

Abstract

Purpose: Develop a 64Cu labeled radiopharmaceutical targeting prostate specific membrane antigen (PSMA) and investigate its application for prostate cancer imaging. Methods: 64Cu-PSMA-BCH was prepared and investigated for stability, PSMA specificity, and micro-PET imaging. With the approval of Ethics Committee of Beijing Cancer Hospital (No. 2017KT97), PET/CT imaging in 4 patients with suspected prostate cancer was performed and the radiation dosimetry was estimated. Then, PSMA PET-ultrasound image-guided biopsies were performed on 3 patients and the fine needle aspirates were further performed for autoradiography and immunohistochemistry analysis. Results: 64Cu-PSMA-BCH was prepared with high radiochemical yield and stability. In vivo study showed higher uptake in PSMA (+) 22Rv1 cells than PSMA (−) PC-3 cells (5.59 ± 0.36 and 1.97 ± 0.22 IA%/106 cells at 1 h). It accumulated in 22Rv1 tumor with increasing radioactivity uptake and T/N ratios from 1 to 24 h post-injection. In patients with suspected prostate cancer, SUVmax and T/N ratios increased within 24 h post-injection. Compared with image at 1 h post-injection, more tumor lesions were detected at 6 h and 24 h post-injection. The human organ radiation dosimetry showed gallbladder wall was most critical, liver and kidneys were followed, and the whole-body effective dose was 0.0292 mSv/MBq. Two fine needle aspirates obtained by PET-ultrasound-guided targeted biopsy showed high radioactive signal by autoradiography, with 100% PSMA expression in cytoplasm and 30% expression in nucleus. Conclusion: 64Cu-PSMA-BCH was PSMA specific and showed high stability in vivo with lower uptake in liver than 64Cu-PSMA-617. Biodistribution in mice and PCa patients showed similar profile compared with other PSMA ligands and it was safe with moderate effective dosimetry. The increased tumor uptake and T/N ratios by delayed imaging may facilitate the detection of small lesions and guiding targeted biopsies.

Original languageEnglish (US)
JournalEuropean Journal of Nuclear Medicine and Molecular Imaging
DOIs
StateAccepted/In press - 2021

Keywords

  • Cu-PSMA
  • Delayed imaging
  • PET/CT
  • Prostate cancer
  • Targeted biopsies

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

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