Therapeutic response and side effects of repeated radioligand therapy with 177Lu-PSMA-DKFZ-617 of castrate-resistant metastatic prostate cancer

Oncotarget. 2016 Mar 15;7(11):12477-88. doi: 10.18632/oncotarget.7245.


Prostate-specific membrane antigen (PSMA) is highly expressed on prostate epithelial cells and strongly up-regulated in prostate cancer (PC), making it an optimal target for the treatment of metastasized PC. Radioligand therapy (RLT) with 177Lu-PSMA-DKFZ-617 (Lu-PSMA) is a targeted therapy for metastatic PC. In this study, we retrospectively analyzed the side effects and the response rate of 24 hormone and/or chemorefractory PC patients with a mean age of 75.2 years (range: 64-82) with distant metastases and progressive disease according to the PSA level, who were treated with Lu-PSMA. Median PSA was 522 ng/ml (range: 17-2360). Forty-six cycles of Lu-PSMA were performed. Of the 24 patients, 22 received two cycles. Eight weeks after the first cycle of Lu-PSMA therapy 79.1% experienced a decline in PSA level. Eight weeks after the second cycle of Lu-PSMA therapy 68.2% experienced a decline in PSA relative to the baseline value. Apart from two cases of grade 3 anemia, there was no relevant hemato- or nephrotoxicity (grade 3 or 4). These results confirmed that Lu-PSMA is a safe treatment option for metastatic PC patients and has a low toxicity profile. A positive response to therapy in terms of decline in PSA occurs in about 70% of patients.

Keywords: 177Lu; PSA; PSMA; prostate cancer; radioligand therapy.

MeSH terms

  • Aged
  • Aged, 80 and over
  • Dipeptides / administration & dosage*
  • Heterocyclic Compounds, 1-Ring / administration & dosage*
  • Humans
  • Lutetium / administration & dosage
  • Lutetium / chemistry
  • Male
  • Middle Aged
  • Organometallic Compounds / administration & dosage*
  • Peptides / administration & dosage*
  • Positron Emission Tomography Computed Tomography
  • Prostate-Specific Antigen
  • Prostatic Neoplasms, Castration-Resistant / diagnostic imaging
  • Prostatic Neoplasms, Castration-Resistant / drug therapy*
  • Prostatic Neoplasms, Castration-Resistant / pathology
  • Prostatic Neoplasms, Castration-Resistant / radiotherapy*
  • Radioisotopes / administration & dosage
  • Radioisotopes / chemistry
  • Radiopharmaceuticals / therapeutic use*
  • Retrospective Studies


  • 177Lu-DKFZ-617
  • 177Lu-PSMA-617
  • Dipeptides
  • Heterocyclic Compounds, 1-Ring
  • Organometallic Compounds
  • Peptides
  • Radioisotopes
  • Radiopharmaceuticals
  • Lutetium
  • Prostate-Specific Antigen