The Theranostic PSMA Ligand PSMA-617 in the Diagnosis of Prostate Cancer by PET/CT: Biodistribution in Humans, Radiation Dosimetry, and First Evaluation of Tumor Lesions

J Nucl Med. 2015 Nov;56(11):1697-705. doi: 10.2967/jnumed.115.161299. Epub 2015 Aug 20.

Abstract

PET imaging with the prostate-specific membrane antigen (PSMA)-targeted radioligand (68)Ga-PSMA-11 is regarded as a significant step forward in the diagnosis of prostate cancer (PCa). More recently, a PSMA ligand was developed that can be labeled with (68)Ga, (111)In, (177)Lu, and (90)Y. This ligand, named PSMA-617, therefore enables both diagnosis and therapy of PCa. The aims of this evaluation were to clinically investigate the distribution of (68)Ga-PSMA-617 in normal tissues and in PCa lesions as well as to evaluate the radiation exposure by the radioligand in PET imaging.

Methods: Nineteen patients, most of them with recurrent PCa, were referred for (68)Ga-PSMA-617 PET/CT. The quantitative assessment of tracer uptake of several organs and of 53 representative tumor lesions was performed in 15 patients at 1 and 3 h after injection. In 4 additional patients, the same procedure was conducted at 5 min, 1 h, 2 h, 3 h, 4 h, and 5 h after injection. On the basis of the data for these 4 patients (mean injected dose, 231 MBq), the radiation exposure of a (68)Ga-PSMA-617 PET/CT was identified.

Results: Intense tracer uptake was observed in the kidneys and salivary glands. In 14 of 19 patients (73.7%), at least 1 lesion suspected of being a tumor was detected at 3 h after injection. Of 53 representative tumor lesions selected at 3 h after injection, 47 lesions were visible at 1 h after injection. The mean tumor-to-background ratio for maximum standardized uptake value was 20.4 ± 17.3 (range, 2.3-84.0) at 1 h after injection and 38.2 ± 38.6 (range, 3.6-154.3) at 3 h after injection. The average radiation exposure (effective dose) was approximately 0.021 mSv/MBq.

Conclusion: Within healthy organs, the kidneys and salivary glands showed the highest (68)Ga-PSMA-617 uptake. The radiation exposure was relatively low. (68)Ga-PSMA-617 shows PCa lesions with high contrast. Images obtained between 2 and 3 h after injection seem to be the best option with regard to radiotracer uptake and tumor contrast. Later images can help to clarify unclear lesions.

Keywords: PET/CT; PSMA; dosimetry; positron emission tomography; prostate cancer; prostate-specific membrane antigen.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Dipeptides / therapeutic use*
  • Edetic Acid / analogs & derivatives
  • Gallium Isotopes
  • Gallium Radioisotopes / therapeutic use*
  • Heterocyclic Compounds, 1-Ring / therapeutic use*
  • Humans
  • Image Processing, Computer-Assisted
  • Kidney / diagnostic imaging
  • Kidney / metabolism
  • Male
  • Middle Aged
  • Oligopeptides
  • Organometallic Compounds / therapeutic use*
  • Positron-Emission Tomography
  • Prostate-Specific Antigen / chemistry*
  • Prostatic Neoplasms / diagnostic imaging*
  • Prostatic Neoplasms / metabolism
  • Prostatic Neoplasms / radiotherapy*
  • Radiometry
  • Radiopharmaceuticals / therapeutic use*
  • Salivary Glands / diagnostic imaging
  • Salivary Glands / metabolism
  • Theranostic Nanomedicine*
  • Tissue Distribution

Substances

  • Dipeptides
  • Gallium Isotopes
  • Gallium Radioisotopes
  • Heterocyclic Compounds, 1-Ring
  • Oligopeptides
  • Organometallic Compounds
  • PSMA-617
  • Radiopharmaceuticals
  • gallium 68 PSMA-11
  • Edetic Acid
  • Prostate-Specific Antigen