Yttrium-90 and indium-111 labelling, receptor binding and biodistribution of [DOTA0,d-Phe1,Tyr3]octreotide, a promising somatostatin analogue for radionuclide therapy

Eur J Nucl Med. 1997 Apr;24(4):368-71. doi: 10.1007/BF00881807.


In vitro octreotide receptor binding of [111In-DOTA0,d-Phe1, Tyr3]octreotide (111In-DOTATOC) and the in vivo metabolism of 90Y- or 111In-labelled DOTATOC were investigated in rats in comparison with [111In-DTPA0]octreotide [111In-DTPAOC). 111In-DOTATOC was found to have an affinity similar to octreotide itself for the octreotide receptor in rat cerebral cortex microsomes. Twenty-four hours after injection of 90Y- or 111In-labelled DOTATOC, uptake of radioactivity in the octreotide receptor-expressing tissues pancreas, pituitary, adrenals and tumour was a factor of 2-6 that after injection of 111In-DTPAOC. Uptake of labelled DOTATOC in pituitary, pancreas, adrenals and tumour was almost completely blocked by pretreatment with 0.5 mg unlabelled octreotide, indicating specific binding to the octreotide receptors. These findings strongly indicate that 90Y-DOTATOC is a promising radiopharmaceutical for radiotherapy and that 111In-DOTATOC is of potential value for diagnosis of patients with octreotide receptor-positive lesions, such as most neuroendocrine tumours.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Indium Radioisotopes / pharmacokinetics*
  • Indium Radioisotopes / therapeutic use
  • Male
  • Octreotide / analogs & derivatives*
  • Octreotide / pharmacokinetics
  • Octreotide / therapeutic use
  • Pentetic Acid / analogs & derivatives
  • Pentetic Acid / pharmacokinetics
  • Pentetic Acid / therapeutic use
  • Radiopharmaceuticals / pharmacokinetics*
  • Radiopharmaceuticals / therapeutic use
  • Rats
  • Rats, Inbred Lew
  • Rats, Wistar
  • Receptors, Somatostatin / metabolism
  • Tissue Distribution
  • Yttrium Radioisotopes / pharmacokinetics*
  • Yttrium Radioisotopes / therapeutic use


  • Indium Radioisotopes
  • Radiopharmaceuticals
  • Receptors, Somatostatin
  • Yttrium Radioisotopes
  • SDZ 215-811
  • Pentetic Acid
  • Octreotide
  • Edotreotide