Tecnetium-99m as alternative to produce somatostatin-labeled derivatives: comparative biodistribution evaluation with 111In-DTPA-octreotide.
Synthetic somatostatin (SST) analogues have been used in the preparation of receptor-specific radiopharmaceuticals for diagnostic and therapy of neuroendocrine tumors. This work studied the labeling conditions with (99m)Tc and biological distribution in Swiss mice of two SST analogs (HYNIC-Tyr(3)-Octreotide and HYNIC-Tyr(3)-Octreotate) and compared the biodistribution pattern with (111)In-DTPA-Octreotide. Biological distribution studies were performed after injection of radiopharmaceuticals on Swiss mice. Labeling procedures resulted on high radiochemical yield for all three preparations and the labeled products presented high in vitro stability. Biological distribution studies evidenced similar general biodistribution of (99m)Tc-labeled peptides when compared with indium-labeled peptide with fast blood clearance and elimination by urinary tract. Kidneys uptake of (99m)Tc-HYNIC-TATE are similar to (111)In-DTPA-Octreotide, and both are significantly higher than (99m)Tc-HYNIC-OCT. All labeled peptides presented similar uptake on liver, but the retention in time at intestines, particularly at large intestine, was more expressive for (111)In-labeled peptide. The %ID of (99m)Tc-HYNIC-OCT and (99m)Tc-HYNIC-TATE in organs with high density of SST receptors like pancreas and adrenals were significant and similar to obtained for (111)In-DTPA-Octreotide, confirming the affinity of these radiopharmaceuticals for the receptors.
Departamento de Radiologia LIM43, Universidade de São Paulo, CEP 05403-010 São Paulo, Brazil. ivani@hcnet.usp.br
I B
IB
Melo
L T
LT
Ueda
E B
EB
Araujo
E
E
Muramoto
M F
MF
Barboz
J
J
Mengatti
C A
CA
Buchpiguel
C P G
CP
Silva
D000818:Animals; D007422:Intestines / Q000000981:diagnostic imaging; D007668:Kidney / Q000187:drug effects; D008024:Ligands; D008099:Liver / Q000000981:diagnostic imaging / Q000187:drug effects; D051379:Mice; D018358:Neuroendocrine Tumors / Q000000981:diagnostic imaging; D015282:Octreotide / Q000737:chemistry; D004369:Pentetic Acid / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D010455:Peptides / Q000737:chemistry; D011786:Quality Control; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000737:chemistry; D013004:Somatostatin / Q000737:chemistry*; D013667:Technetium / Q000493:pharmacokinetics*; D013997:Time Factors; D014018:Tissue Distribution
C442550:(111)indium-DTPA-D-phe octreoide; D008024:Ligands; D010455:Peptides; D019275:Radiopharmaceuticals; D013004:Somatostatin; D013667:Technetium; D004369:Pentetic Acid; D015282:Octreotide