PET imaging with a [68Ga]gallium-labelled PSMA ligand for the diagnosis of prostate cancer: biodistribution in humans and first evaluation of tumour lesions

Eur J Nucl Med Mol Imaging. 2013 Apr;40(4):486-95. doi: 10.1007/s00259-012-2298-2. Epub 2012 Nov 24.


Purpose: Prostate-specific membrane antigen (PSMA) is a cell surface protein with high expression in prostate carcinoma (PC) cells. Recently, procedures have been developed to label PSMA ligands with (68)Ga, (99m)Tc and (123/124/131)I. Our initial experience with Glu-NH-CO-NH-Lys-(Ahx)-[(68)Ga(HBED-CC)]((68)Ga-PSMA) suggests that this novel tracer can detect PC relapses and metastases with high contrast. The aim of this study was to investigate its biodistribution in normal tissues and tumour lesions.

Methods: A total of 37 patients with PC and rising prostate-specific antigen (PSA) levels were subjected to (68)Ga-PSMA positron emission tomography (PET)/CT. Quantitative assessment of tracer uptake was performed 1 and 3 h post-injection (p.i.) by analysis of mean and maximum standardized uptake values (SUVmean/max) of several organs and 65 tumour lesions. Subsequently, tumour to background ratios were calculated.

Results: The PET/CT images showed intense tracer uptake in both kidneys and salivary glands. Moderate uptake was seen in lacrimal glands, liver, spleen and in small and large bowel. Quantitative assessment revealed excellent contrast between tumour lesions and most normal tissues. Of 37 patients, 31 (83.8 %) showed at least one lesion suspicious for cancer at a detection rate of 60 % at PSA <2.2 ng/ml and 100 % at PSA >2.2 ng/ml. Median tumour to background ratios were 18.8 (2.4-158.3) in early images and 28.3 (2.9-224.0) in late images.

Conclusion: The biodistribution of the novel (68)Ga-PSMA tracer and its ability to detect PC lesions was analysed in 37 patients. Within healthy organs, kidneys and salivary glands demonstrated the highest radiotracer uptake. Lesions suspicious for PC presented with excellent contrast as early as 1 h p.i. with high detection rates even at low PSA levels.

MeSH terms

  • Aged
  • Aged, 80 and over
  • Antigens, Surface / analysis*
  • Carcinoma / diagnostic imaging*
  • Edetic Acid / analogs & derivatives*
  • Edetic Acid / pharmacokinetics
  • Gallium Isotopes
  • Gallium Radioisotopes* / pharmacokinetics
  • Glutamate Carboxypeptidase II / analysis*
  • Humans
  • Ligands
  • Male
  • Middle Aged
  • Multimodal Imaging*
  • Oligopeptides* / pharmacokinetics
  • Positron-Emission Tomography*
  • Prostatic Neoplasms / diagnostic imaging*
  • Radiopharmaceuticals* / pharmacokinetics
  • Tissue Distribution
  • Tomography, X-Ray Computed*


  • Antigens, Surface
  • Gallium Isotopes
  • Gallium Radioisotopes
  • Ligands
  • Oligopeptides
  • Radiopharmaceuticals
  • gallium 68 PSMA-11
  • Edetic Acid
  • FOLH1 protein, human
  • Glutamate Carboxypeptidase II