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

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 octreo...

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Bibliographic Details
Published in:European Journal of Nuclear Medicine 1997-04, Vol.24 (4), p.368-371
Main Authors: DE JONG, M, BAKKER, W. H, MÄCKE, H. R, KRENNING, E. P, BREEMAN, W. A. P, VAN DER PLUIJM, M. E, BERNARD, B. F, VISSER, T. J, JERMANN, E, BEHE, M, POWELL, P
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Contrast media. Radiopharmaceuticals
Indium Radioisotopes - pharmacokinetics
Indium Radioisotopes - therapeutic use
Male
Medical sciences
Octreotide - analogs & derivatives
Octreotide - pharmacokinetics
Octreotide - therapeutic use
Pentetic Acid - analogs & derivatives
Pentetic Acid - pharmacokinetics
Pentetic Acid - therapeutic use
Pharmacology. Drug treatments
Radiopharmaceuticals - pharmacokinetics
Radiopharmaceuticals - therapeutic use
Rats
Rats, Inbred Lew
Rats, Wistar
Receptors, Somatostatin - metabolism
Tissue Distribution
Yttrium Radioisotopes - pharmacokinetics
Yttrium Radioisotopes - therapeutic use
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Summary: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.
ISSN:0340-6997
1619-7089
DOI:10.1007/BF00881807