title: Biokinetics of 111In-DTPA-D-Phe(1)-octreotide in nude mice transplanted with a human carcinoid tumor.
abstract: The long time biokinetics of the radiolabeled somatostatin analogues 111In-DTPA-D-Phe(1)-octreotide was studied in nude mice transplanted with the human carcinoid tumor, GOT1. The results were compared with those from the patient with the original tumor. This patient has been diagnosed and later treated with 111In-DTPA-D-Phe(1)-octreotide. The animals received about 2 MBq 111In-DTPA-D-Phe(1)-octreotide (0.1 microg) by injection into a tail vein. The animals were killed 0.5 h-14 d after injection of the radiopharmaceutical. Tumor tissue and normal tissues were collected and weighed and measured for 111In activity. The 111In uptake in the tumor was higher than in all normal tissues except the kidneys. The tumor-to-normal-tissue activity concentration, TNC, increased with time for all normal tissues studied. These data were similar to those observed for the original tumor in the patient. The similar biokinetics for 111In-DTPA-D-Phe(1)-octreotide in the tumor-bearing mice and the patient makes this animal model suitable as a model for evaluation of therapy of somatostatin receptor (sstr) expressing tumors with radiolabeled somatostatin analogues. Furthermore, the increase with time of TNC both in mice and the patient indicates that long-lived radionuclides are preferred for therapy with radiolabeled somatostatin analogues.
authors.affiliation: Department of Radiation Physics, the Lundberg Laboratory for Cancer Research, Göteborg University, Sahlgrenska University Hospital, S-413 45, Göteborg, Sweden. peter.bernhardt@radfys.gu.se
authors.forename: P
authors.initials: P
authors.lastname: Bernhardt
authors.forename: L
authors.initials: L
authors.lastname: Kölby
authors.forename: V
authors.initials: V
authors.lastname: Johanson
authors.forename: S A
authors.initials: SA
authors.lastname: Benjegård
authors.forename: O
authors.initials: O
authors.lastname: Nilsson
authors.forename: H
authors.initials: H
authors.lastname: Ahlman
authors.forename: E
authors.initials: E
authors.lastname: Forssell-Aronsson
mesh_terms: D000818:Animals; D002276:Carcinoid Tumor / Q000000981:diagnostic imaging / Q000188:drug therapy / Q000378:metabolism*; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D051379:Mice; D008819:Mice, Nude; D009368:Neoplasm Transplantation; D015282:Octreotide / Q000031:analogs & derivatives* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D004369:Pentetic Acid / Q000031:analogs & derivatives* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics* / Q000627:therapeutic use; D014018:Tissue Distribution
chemical_list: D019275:Radiopharmaceuticals; C071632:SDZ 215-811; D004369:Pentetic Acid; D015282:Octreotide