Radiolabeled somatostatin analogs in prostate cancer

Vapreotide (RC-160), a somatostatin analog, was labeled with 99mTc by a direct method and also by using CPTA [1,4,8,11-tetraazacyclotetradecane]as a bifunctional chelating agent. The labeled compounds were evaluated in nude mice bearing experimental human prostate cancers. In these studies, 111In-DT...

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Bibliographic Details
Published in:Nuclear medicine and biology 1997, Vol.24 (1), p.105-113
Main Authors: Thakur, M.L., Kolan, H., Li, J., Wiaderkiewicz, R., Pallela, V.R., Duggaraju, R., Schally, A.V.
Format: Article
Language:English
Subjects:
99mTc labeled octreotide
99mTc labeled RC-160
Animals
Antineoplastic Agents - pharmacokinetics
Antineoplastic Agents, Hormonal - pharmacokinetics
Biological and medical sciences
Humans
Imaging prostate cancer
Male
Medical sciences
Mice
Mice, Nude
Nephrology. Urinary tract diseases
Octreotide - pharmacokinetics
Oxytocin - pharmacology
Prostatic Neoplasms - diagnostic imaging
Prostatic Neoplasms - metabolism
Radiolabeled Somatostatin analogs
Radionuclide Imaging
Receptor specific peptides in prostate cancer
Receptors, Somatostatin - metabolism
Somatostatin - analogs & derivatives
Somatostatin - pharmacokinetics
Technetium Compounds - pharmacokinetics
Tissue Distribution
Tumor Cells, Cultured - metabolism
Tumors of the urinary system
Urinary tract. Prostate gland
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Description
Summary:Vapreotide (RC-160), a somatostatin analog, was labeled with 99mTc by a direct method and also by using CPTA [1,4,8,11-tetraazacyclotetradecane]as a bifunctional chelating agent. The labeled compounds were evaluated in nude mice bearing experimental human prostate cancers. In these studies, 111In-DTPA-D-Phe-Octreotide ( 111In-DTPA-octreotide) served as a standard and 99mTc-oxytocin as a receptornon-specific control. 99mTc-octreotide was also used. The 24 htumor uptake of 99mTc-RC-160 was nearly 400% higher, ( p < 0.05), than that of 111In-DTPA-octreotide and diminished upon receptor blocking. In all tissues except the kidneys, the uptake of 99mTc-RC-160 was also higher than that of 111In-DTPA-octreotide. The uptake of 99mTc-RC-160 was influenced by the amount of peptide injected and the best tumor/muscle and tumor/blood ratios were obtained when only one μg of the peptide (200 Ci/mmol) was administered.
ISSN:0969-8051
1872-9614
DOI:10.1016/S0969-8051(96)00180-1