[177Lu-DOTAOTyr3]octreotate: comparison with [111In-DTPAo]octreotide in patients

Eur J Nucl Med. 2001 Sep;28(9):1319-25. doi: 10.1007/s002590100574.


The somatostatin analogue [DOTA0,Tyr3]octreotate has a nine-fold higher affinity for the somatostatin receptor subtype 2 as compared with [DOTA0, Tyr3]octreotide. Also, labelled with the beta- and gamma-emitting radionuclide lutetium-177, this compound has been shown to have a very favourable impact on tumour regression and animal survival in a rat model. Because of these reported advantages over the analogues currently used for somatostatin receptor-mediated radiotherapy, we decided to compare [177Lu-DOTA0,Tyr3]octreotate (177Lu-octreotate) with [111In-DTPA0]octreotide (111In-octreotide) in six patients with somatostatin receptor-positive tumours. Plasma radioactivity after 177Lu-octreotate expressed as a percentage of the injected dose was comparable with that after 111In-octreotide. Urinary excretion of radioactivity was significantly lower than after 111In-octreotide, averaging 64% after 24 h. The uptake after 24 h, expressed as a percentage of the injected dose of 177Lu-octreotate, was comparable to that after 111In-octreotide for kidneys, spleen and liver, but was three- to fourfold higher for four of five tumours. The spleen and kidneys received the highest absorbed doses. The doses to the kidneys were reduced by a mean of 47% after co-infusion of amino acids. It is concluded that in comparison with the radionuclide-coupled somatostatin analogues that are currently available for somatostatin receptor-mediated radiotherapy, 177Lu-octreotate potentially represents an important improvement. Higher absorbed doses can be achieved to most tumours, with about equal doses to potentially dose-limiting organs; furthermore, the lower tissue penetration range of 177Lu as compared with 90Y may be especially important for small tumours.

Publication types

  • Comparative Study

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Female
  • Humans
  • Indium Radioisotopes* / pharmacokinetics
  • Lutetium* / pharmacokinetics
  • Male
  • Middle Aged
  • Neoplasms / chemistry
  • Neoplasms / diagnostic imaging*
  • Neoplasms / radiotherapy
  • Octreotide / analogs & derivatives
  • Organometallic Compounds* / pharmacokinetics
  • Radiation Dosage
  • Radioisotopes* / pharmacokinetics
  • Radionuclide Imaging
  • Radiopharmaceuticals* / pharmacokinetics
  • Radiopharmaceuticals* / therapeutic use
  • Receptors, Somatostatin / analysis*
  • Somatostatin* / analogs & derivatives
  • Somatostatin* / pharmacokinetics


  • Indium Radioisotopes
  • Organometallic Compounds
  • Radioisotopes
  • Radiopharmaceuticals
  • Receptors, Somatostatin
  • Somatostatin
  • Lutetium
  • lutetium Lu 177 dotatate
  • pentetreotide
  • Octreotide