Synthesis and evaluation of [(64)Cu]PSMA-617 targeted for prostate-specific membrane antigen in prostate cancer.

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Synthesis and evaluation of [(64)Cu]PSMA-617 targeted for prostate-specific membrane antigen in prostate cancer.

Am J Nucl Med Mol Imaging. 2017;7(2):40-52

Authors: Cui C, Hanyu M, Hatori A, Zhang Y, Xie L, Ohya T, Fukada M, Suzuki H, Nagatsu K, Jiang C, Luo R, Shao G, Zhang M, Wang F

Abstract
We radiolabeled a ligand, PSMA-617, of prostate-specific membrane antigen (PSMA) with copper-64 ((64)Cu), to evaluate the metabolism, biodistribution, and potential of [(64)Cu]PSMA-617 for PET imaging of prostate cancer. [(64)Cu]PSMA-617 was synthesized by heating PSMA-617 with [(64)Cu]CuCl2 in buffer solution at 90°C for 5 min. In vitro uptake was determined in two cell lines of prostate cancer. In vivo regional distributions were determined in normal and tumor-bearing mice. High radiolabeling efficiency of (64)Cu for PSMA-617 yielded [(64)Cu]PSMA-617 with >99% radiochemical purity. In vitro cellular uptake experiments demonstrated the specificity of [(64)Cu]PSMA-617 for PSMA-positive LNCaP cells. Biodistribution observations of normal mice revealed high uptake of radioactivity in the kidney and liver. PET with [(64)Cu]PSMA-617 visualized tumor areas implanted by PSMA-positive LNCaP cells in the mice. Two hours after the injection of [(64)Cu]PSMA-617 into mice, a radiolabeled metabolite was observed in the blood, liver, urine, and LNCaP tumor tissues. [(64)Cu]PSMA-617 was easily synthesized, and exhibited a favorable biodistribution in PSMA-positive tumors. Although this radioligand shows slow clearance for kidney and high liver uptake, change of its chelator moiety and easy radiolabeling may enable development of new (64)Cu or (67)Cu-labeled PSMA ligands for imaging and radiotherapy.

PMID: 28533936 [PubMed]

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