Radiolabelled somatostatin analogue(s) for peptide receptor scintigraphy and radionuclide therapy

Ann Oncol. 1999:10 Suppl 2:S23-9. doi: 10.1093/annonc/10.suppl_2.s23.

Abstract

Background: Peptide receptor scintigraphy with the radioactive somatostatin analogue, [111In-DTPA0]octreotide, is a sensitive and specific technique to show in vivo the presence and abundance of somatostatin receptors on various tumours.

Aim: With this technique primary tumours and metastases of neuroendocrine cancers as well as of many other cancer-types can be localised. This technique is currently used to assess the possibility of peptide receptor radionuclide therapy (PRRT) with repeated administrations of high doses of [111In-DTPA0)octreotide. 111In emits Auger and conversion electrons having a tissue penetration of 0.02-10 microns and 200 to 500 microns, respectively.

Patients and methods: Thirty end-stage patients with mostly neuroendocrine progressing tumours were treated with [111In-DTPA0]octreotide, up to a maximal cumulative patient dose of about 74 GBq, in a phase I trial.

Results: There were no major clinical side effects after up to two years treatment, except that in a few patients a transient decline in platelets counts and lymphocyte subsets occurred. Promising beneficial effects on clinical symptoms, hormone production and tumour proliferation were found. Of the 21 patients who received a cumulative dose of more than 20 GBq, eight patients showed stabilisation of disease and six other patients a reduction in size of tumours. There is a tendency towards better results in patients whose tumours have a higher accumulation of the radioligand.

Conclusions: PRRT is feasible, also with 111In as radionuclide. Depending on the homogeneity of distribution of tumour cells expressing peptide receptors and the size of the tumour, beta-emitting radionuclides, e.g., 90Y, labelled to DOTA-chelated peptides, are also attractive candidates for PRRT. The first PRRT trials with [90Y-DOTA0,Tyr3]octreotide started recently.

Publication types

  • Clinical Trial
  • Clinical Trial, Phase I

MeSH terms

  • Animals
  • Humans
  • Indium Radioisotopes / pharmacokinetics
  • Indium Radioisotopes / therapeutic use*
  • Liver Neoplasms / diagnosis
  • Liver Neoplasms / metabolism
  • Liver Neoplasms / radiotherapy
  • Liver Neoplasms / secondary
  • Neuroendocrine Tumors / diagnosis
  • Neuroendocrine Tumors / metabolism
  • Neuroendocrine Tumors / pathology
  • Neuroendocrine Tumors / radiotherapy*
  • Octreotide / adverse effects
  • Octreotide / analogs & derivatives*
  • Octreotide / pharmacokinetics
  • Octreotide / therapeutic use
  • Pentetic Acid / adverse effects
  • Pentetic Acid / analogs & derivatives*
  • Pentetic Acid / pharmacokinetics
  • Pentetic Acid / therapeutic use
  • Radiopharmaceuticals / adverse effects
  • Radiopharmaceuticals / pharmacokinetics
  • Radiopharmaceuticals / therapeutic use*
  • Rats
  • Receptors, Peptide / analysis*
  • Receptors, Peptide / metabolism
  • Receptors, Somatostatin / analysis
  • Receptors, Somatostatin / metabolism

Substances

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