Source:http://linkedlifedata.com/resource/pubmed/id/12552352
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2003-1-28
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pubmed:abstractText |
Peptide receptor-targeted radionuclide therapy is nowadays also being performed with DOTA-conjugated peptides, such as [DOTA(0),Tyr(3)]octreotate, labelled with radionuclides like (177)Lu. The incorporation of (177)Lu is typically >/=99.5%; however, since a total patient dose can be as high as 800 mCi, the amount of free (177)Lu(3+) (= non-DOTA-incorporated) can be substantial. Free (177)Lu(3+) accumulates in bone with unwanted irradiation of bone marrow as a consequence. (177)Lu-DTPA is reported to be stable in serum in vitro, and in vivo it has rapid renal excretion. Transforming free Lu(3+) to Lu-DTPA might reroute this fraction from accumulation in bone to renal clearance. We therefore investigated: (a) the biodistribution in rats of (177)LuCl(3), [(177)Lu-DOTA(0),Tyr(3)]octreotate and (177)Lu-DTPA; (b) the possibilities of complexing the free (177)Lu(3+) in [(177)Lu-DOTA(0),Tyr(3)]octreotate to (177)Lu-DTPA prior to intravenous injection; and (c) the effects of free (177)Lu(3+) in [(177)Lu-DOTA(0),Tyr(3)]octreotate, in the presence and absence of DTPA, on the biodistribution in rats. (177)LuCl(3) had high skeletal uptake (i.e. 5% ID per gram femur, with localization mainly in the epiphyseal plates) and a 24-h total body retention of 80% injected dose (ID). [(177)Lu-DOTA(0),Tyr(3)]octreotate had high and specific uptake in somatostatin receptor-positive tissues, and 24-h total body retention of 19% ID. (177)Lu-DTPA had rapid renal clearance, and 24-h total body retention of 4% ID. Free (177)Lu(3+) in [(177)Lu-DOTA(0),Tyr(3)]octreotate could be complexed to (177)Lu-DTPA. Accumulation of (177)Lu in femur, blood, liver and spleen showed a dose relation to the amount of free (177)Lu(3+), while these accumulations could be normalized by the addition of DTPA. After labelling [DOTA(0),Tyr(3)]octreotate with (177)Lu the addition of DTPA prior to intravenous administration of [(177)Lu-DOTA(0),Tyr(3)]octreotate is strongly recommended.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/(177lutetium-DOTA(O)Tyr3)octreotate,
http://linkedlifedata.com/resource/pubmed/chemical/1,4,7,10-tetraazacyclododecane-...,
http://linkedlifedata.com/resource/pubmed/chemical/Heterocyclic Compounds, 1-Ring,
http://linkedlifedata.com/resource/pubmed/chemical/Lutetium,
http://linkedlifedata.com/resource/pubmed/chemical/Octreotide,
http://linkedlifedata.com/resource/pubmed/chemical/Organometallic Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Pentetic Acid,
http://linkedlifedata.com/resource/pubmed/chemical/Radiation-Protective Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Radiopharmaceuticals
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
1619-7070
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
30
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
312-5
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:12552352-Animals,
pubmed-meshheading:12552352-Bone Marrow,
pubmed-meshheading:12552352-Femur,
pubmed-meshheading:12552352-Heterocyclic Compounds, 1-Ring,
pubmed-meshheading:12552352-Injections, Intravenous,
pubmed-meshheading:12552352-Kidney,
pubmed-meshheading:12552352-Lutetium,
pubmed-meshheading:12552352-Male,
pubmed-meshheading:12552352-Octreotide,
pubmed-meshheading:12552352-Organ Specificity,
pubmed-meshheading:12552352-Organometallic Compounds,
pubmed-meshheading:12552352-Pentetic Acid,
pubmed-meshheading:12552352-Radiation-Protective Agents,
pubmed-meshheading:12552352-Radioisotopes,
pubmed-meshheading:12552352-Radiometry,
pubmed-meshheading:12552352-Radiopharmaceuticals,
pubmed-meshheading:12552352-Rats,
pubmed-meshheading:12552352-Rats, Wistar,
pubmed-meshheading:12552352-Tissue Distribution
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pubmed:year |
2003
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pubmed:articleTitle |
The addition of DTPA to [177Lu-DOTA0,Tyr3]octreotate prior to administration reduces rat skeleton uptake of radioactivity.
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pubmed:affiliation |
Department of Nuclear Medicine, Erasmus University Medical Center, Dr. Molewaterplein 40, 3015 GD Rotterdam, The Netherlands. breeman@nuge.azr.nl
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pubmed:publicationType |
Journal Article,
Comparative Study,
Evaluation Studies
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