Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
2003-1-28
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.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Feb
pubmed:issn
1619-7070
pubmed:author
pubmed:issnType
Print
pubmed:volume
30
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
312-5
pubmed:dateRevised
2007-11-15
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
pubmed:year
2003
pubmed:articleTitle
The addition of DTPA to [177Lu-DOTA0,Tyr3]octreotate prior to administration reduces rat skeleton uptake of radioactivity.
pubmed:affiliation
Department of Nuclear Medicine, Erasmus University Medical Center, Dr. Molewaterplein 40, 3015 GD Rotterdam, The Netherlands. breeman@nuge.azr.nl
pubmed:publicationType
Journal Article, Comparative Study, Evaluation Studies