title: A new radiolabelled somatostatin analogue [111In-DTPA-D-Phe1]RC-160: preparation, biological activity, receptor scintigraphy in rats and comparison with [111In-DTPA-D-Phe1]octreotide.
abstract: We have evaluated the potential usefulness of indium-111 labelled [DTPA-D-Phe1]RC-160, derived from the octapeptide somatostatin analogue RC-160, as a radiopharmaceutical for the in vivo detection of somatostatin receptor-positive tumours. For this purpose 111In-and 115In-labelled [DTPA-D-Phe1]RC-160 was tested for its biological activity, and applied for somatostatin receptor scintigraphy in vivo to rats bearing the transplantable rat pancreatic tumour CA20948, which expresses somatostatin receptors. We previously described the development of the 111In-labelled somatostatin analogue [DTPA-D-Phe1]octreotide and its use in the in vivo visualization of somatostatin receptor-positive tumours in rats and in humans. Like [111In-DTPA-D-Phe1]octreotide, [111In-DTPA-D-Phe1]RC-160 showed uptake in and specific binding in vivo to somatostatin receptor-positive organs and tumours, and the tumours were clearly visualized by gamma camera scintigraphy. However, as compared to [111In-DTPA-D-Phe1]octreotide, blood radioactivity (background) was higher, resulting in a lower tumour to blood (background) ratio. Using this animal model we therefore conclude that [111In-DTPA-D-Phe1]RC-160 has no advantage over [111In-DTPA-D-Phe1]octreotide as a radiopharmaceutical in the visualization of somatostatin receptors which bind both analogues. However, recent reports suggest the existence of different somatostatin receptor subtypes on some human cancers, which differentially bind RC-160 and not octreotide. These tumours include cancers of the breast, ovary, exocrine pancreas, prostate and colon. [111In-DTPA-D-Phe1]RC-160 might be of interest for future use in such cancer patients as a radiopharmaceutical for imaging somatostatin receptor-positive tumours, which do not bind octreotide.
authors.affiliation: Department of Nuclear Medicine, University Hospital Dijkzigt, Rotterdam, The Netherlands.
authors.forename: W A
authors.initials: WA
authors.lastname: Breeman
authors.forename: L J
authors.initials: LJ
authors.lastname: Hofland
authors.forename: M
authors.initials: M
authors.lastname: van der Pluijm
authors.forename: P M
authors.initials: PM
authors.lastname: van Koetsveld
authors.forename: M
authors.initials: M
authors.lastname: de Jong
authors.forename: B
authors.initials: B
authors.lastname: Setyono-Han
authors.forename: W H
authors.initials: WH
authors.lastname: Bakker
authors.forename: D J
authors.initials: DJ
authors.lastname: Kwekkeboom
authors.forename: T J
authors.initials: TJ
authors.lastname: Visser
authors.forename: S W
authors.initials: SW
authors.lastname: Lamberts
mesh_terms: D000818:Animals; D007205:Indium Radioisotopes; D008297:Male; D015282:Octreotide / Q000031:analogs & derivatives*; D010190:Pancreatic Neoplasms / Q000737:chemistry / Q000000981:diagnostic imaging*; D004369:Pentetic Acid / Q000031:analogs & derivatives*; D011877:Radionuclide Imaging; D051381:Rats; D011917:Rats, Inbred Lew; D017481:Receptors, Somatostatin / Q000032:analysis; D013004:Somatostatin / Q000031:analogs & derivatives*; D014018:Tissue Distribution
chemical_list: D007205:Indium Radioisotopes; D017481:Receptors, Somatostatin; C071632:SDZ 215-811; C051458:vapreotide; D013004:Somatostatin; D004369:Pentetic Acid; D015282:Octreotide