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. Epub 2019 Jan 17.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Gallium / chemistry*
  • Gallium / pharmacology
  • Humans
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Molecular Structure
  • Neoplasms, Experimental / diagnostic imaging*
  • Prostatic Neoplasms / diagnostic imaging*
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / pharmacology

Substances

  • Radiopharmaceuticals
  • Gallium