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

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%. 68 Ga-PSMA-BCH was obtained by radiolabeling NOTA-PSMA with 68 GaCl 3 with >99% radiochemical purity and 59–74 GBq/μmol specific activity. In vitro and in vivo study of 68 Ga-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 68 Ga-PSMA-617, 68 Ga-PSMA-BCH showed comparable tumor uptake and tumor-background ratios. Indicating 68 Ga-PSMA-BCH is a promising candidate for prostate cancer imaging and worthy of further clinical investigations.