Synthesis and preclinical evaluation of 68Ga-PSMA-BCH for prostate cancer imaging

  • Bioorg Med Chem Lett. 2019 Apr 1;29(7):933-937. doi: 10.1016/j.bmcl.2019.01.013.
Teli Liu  1 ,  Chen Liu  1 ,  Fei Liu  1 ,  Xiaoxia Xu  1 ,  Xiaoyi Guo  1 ,  Lei Xia  1 ,  Hua Zhu  2 ,  Zhi Yang  3
Affiliations
  • 1. Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing 100142, PR China.
  • 2. Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing 100142, PR China. Electronic address: [email protected].
  • 3. Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing 100142, PR China. Electronic address: [email protected].
PMID: 30745258 DOI: 10.1016/j.bmcl.2019.01.013
Abstract

Prostate specific membrane antigen (PSMA) is a promising target for the diagnosis and therapy of prostate Cancer. In this report, a NOTA-conjugated precursor, NOTA-PSMA (also named PSMA-BCH), was synthesized by peptide synthesizer with the chemical purity over 95%. 68Ga-PSMA-BCH was obtained by radiolabeling NOTA-PSMA with 68GaCl3 with >99% radiochemical purity and 59-74 GBq/μmol specific activity. In vitro and in vivo study of 68Ga-PSMA-BCH showed high stability, high uptake in PSMA-expressing cells and tumor, fast clearance and low non-target uptake. 22Rv1 tumors were clearly observed in micro-PET images of and showed good retention. Compared with 68Ga-PSMA-617, 68Ga-PSMA-BCH showed comparable tumor uptake and tumor-background ratios. Indicating 68Ga-PSMA-BCH is a promising candidate for prostate Cancer imaging and worthy of further clinical investigations.

Keywords
(68)Ga-PSMA-BCH; PET imaging; PSMA; Prostate cancer.
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