Comparison of [(177)Lu-DOTA(0),Tyr(3)]octreotate and [(177)Lu-DOTA(0),Tyr(3)]octreotide: which peptide is preferable for PRRT?

Eur J Nucl Med Mol Imaging. 2006 Nov;33(11):1346-51. doi: 10.1007/s00259-006-0172-9. Epub 2006 Jul 18.

Abstract

Purpose: Patients with somatostatin receptor subtype 2-positive metastasised neuroendocrine tumours can be treated with [(177)Lu-DOTA(0),Tyr(3)]octreotate. Some use octreotide as the peptide for peptide receptor radionuclide therapy (PRRT). We compared in seven patients [(177)Lu-DOTA(0),Tyr(3)]octreotide ((177)Lu-DOTATOC) and [(177)Lu-DOTA(0),Tyr(3)]octreotate ((177)Lu-DOTATATE), to see which peptide should be preferred for PRRT with (177)Lu.

Methods: In the same patients, 3,700 MBq (177)Lu-DOTATOC and 3,700 MBq (177)Lu-DOTATATE was administered in separate therapy sessions. Amino acids were co-administered. Whole-body scanning was performed on days 1, 4 and 7 post therapy. Blood and urine samples were collected. We calculated residence times for tumours, spleen and kidneys.

Results: All patients had longer residence times in spleen, kidneys and tumours after use of (177)Lu-DOTATATE (p=0.016 in each case). Comparing (177)Lu-DOTATATE with (177)Lu-DOTATOC, the mean residence time ratio was 2.1 for tumour, 1.5 for spleen and 1.4 for kidneys. Dose-limiting factors for PRRT are bone marrow and/or kidney dose. Although the residence time for kidneys was longer when using (177)Lu-DOTATATE, the mean administered dose to tumours would still be advantageous by a factor of 1.5, assuming a fixed maximum kidney dose is reached. Plasma radioactivity after (177)Lu-DOTATATE was comparable to that after (177)Lu-DOTATOC. Urinary excretion of radioactivity was comparable during the first 6 h; thereafter there was a significant advantage for (177)Lu-DOTATOC.

Conclusion: (177)Lu-DOTATATE had a longer tumour residence time than (177)Lu-DOTATOC. Despite a longer residence time in kidneys after (177)Lu-DOTATATE, tumour dose will always be higher. Therefore, we conclude that the better peptide for PRRT is octreotate.

Publication types

  • Clinical Trial
  • Comparative Study

MeSH terms

  • Adult
  • Aged
  • Female
  • Humans
  • Male
  • Metabolic Clearance Rate
  • Middle Aged
  • Neuroendocrine Tumors / metabolism*
  • Neuroendocrine Tumors / radiotherapy*
  • Octreotide / analogs & derivatives*
  • Octreotide / pharmacokinetics
  • Octreotide / therapeutic use
  • Organ Specificity
  • Organometallic Compounds / pharmacokinetics*
  • Organometallic Compounds / therapeutic use*
  • Radiopharmaceuticals / pharmacokinetics
  • Radiopharmaceuticals / therapeutic use
  • Tissue Distribution

Substances

  • 177Lu-octreotide, DOTA(0)-Tyr(3)-
  • Organometallic Compounds
  • Radiopharmaceuticals
  • lutetium Lu 177 dotatate
  • Octreotide