Comprehensive evaluation of a somatostatin-based radiolabelled antagonist for diagnostic imaging and radionuclide therapy.
Identifieur interne : 000F36 ( Main/Exploration ); précédent : 000F35; suivant : 000F37Comprehensive evaluation of a somatostatin-based radiolabelled antagonist for diagnostic imaging and radionuclide therapy.
Auteurs : RBID : pubmed:22926735English descriptors
- KwdEn :
- Animals, Female, HEK293 Cells, Humans, Indium Radioisotopes (diagnostic use), Indium Radioisotopes (metabolism), Indium Radioisotopes (pharmacokinetics), Indium Radioisotopes (therapeutic use), Lutetium (diagnostic use), Lutetium (metabolism), Lutetium (pharmacokinetics), Lutetium (therapeutic use), Mice, Mice, Nude, Neoplasm Transplantation, Neoplasms (radionuclide imaging), Neoplasms (radiotherapy), Octreotide (diagnostic use), Octreotide (metabolism), Octreotide (pharmacokinetics), Octreotide (therapeutic use), Organometallic Compounds (diagnostic use), Organometallic Compounds (metabolism), Organometallic Compounds (pharmacokinetics), Organometallic Compounds (therapeutic use), Radiopharmaceuticals (diagnostic use), Radiopharmaceuticals (metabolism), Radiopharmaceuticals (pharmacokinetics), Radiopharmaceuticals (therapeutic use), Receptors, Somatostatin (antagonists & inhibitors), Receptors, Somatostatin (metabolism), Tissue Distribution.
- MESH :
- chemical , antagonists & inhibitors : Receptors, Somatostatin.
- chemical , diagnostic use : Indium Radioisotopes, Lutetium, Octreotide, Organometallic Compounds, Radiopharmaceuticals.
- chemical , metabolism : Indium Radioisotopes, Lutetium, Octreotide, Organometallic Compounds, Radiopharmaceuticals, Receptors, Somatostatin.
- chemical , pharmacokinetics : Indium Radioisotopes, Lutetium, Octreotide, Organometallic Compounds, Radiopharmaceuticals.
- chemical , therapeutic use : Indium Radioisotopes, Lutetium, Octreotide, Organometallic Compounds, Radiopharmaceuticals.
- radionuclide imaging : Neoplasms.
- radiotherapy : Neoplasms.
- Animals, Female, HEK293 Cells, Humans, Mice, Mice, Nude, Neoplasm Transplantation, Tissue Distribution.
Abstract
Targeting of tumours positive for somatostatin receptors (sst) with radiolabelled peptides is of interest for tumour localization, staging, therapy follow-up and targeted radionuclide therapy. The peptides used clinically are exclusively agonists, but recently we have shown that the radiolabelled somatostatin-based antagonist (111)In-DOTA-sst2-ANT may be preferable to agonists. However, a comprehensive study of this radiolabelled antagonist to determine its significance was lacking. The present report describes the evaluation of this novel antagonist labelled with (111)In and (177)Lu in three different tumour models.
DOI: 10.1007/s00259-012-2231-8
PubMed: 22926735
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Comprehensive evaluation of a somatostatin-based radiolabelled antagonist for diagnostic imaging and radionuclide therapy.</title><author><name sortKey="Wang, Xuejuan" uniqKey="Wang X">Xuejuan Wang</name><affiliation wicri:level="1"><nlm:affiliation>Division of Radiological Chemistry, University Hospital Basel, Switzerland.</nlm:affiliation><country xml:lang="fr">Suisse</country><wicri:regionArea>Division of Radiological Chemistry, University Hospital Basel</wicri:regionArea></affiliation></author><author><name sortKey="Fani, Melpomeni" uniqKey="Fani M">Melpomeni Fani</name></author><author><name sortKey="Schulz, Stefan" uniqKey="Schulz S">Stefan Schulz</name></author><author><name sortKey="Rivier, Jean" uniqKey="Rivier J">Jean Rivier</name></author><author><name sortKey="Reubi, Jean Claude" uniqKey="Reubi J">Jean Claude Reubi</name></author><author><name sortKey="Maecke, Helmut R" uniqKey="Maecke H">Helmut R Maecke</name></author></titleStmt><publicationStmt><date when="2012">2012</date><idno type="doi">10.1007/s00259-012-2231-8</idno><idno type="RBID">pubmed:22926735</idno><idno type="pmid">22926735</idno><idno type="wicri:Area/Main/Corpus">000B05</idno><idno type="wicri:Area/Main/Curation">000B05</idno><idno type="wicri:Area/Main/Exploration">000F36</idno></publicationStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Female</term><term>HEK293 Cells</term><term>Humans</term><term>Indium Radioisotopes (diagnostic use)</term><term>Indium Radioisotopes (metabolism)</term><term>Indium Radioisotopes (pharmacokinetics)</term><term>Indium Radioisotopes (therapeutic use)</term><term>Lutetium (diagnostic use)</term><term>Lutetium (metabolism)</term><term>Lutetium (pharmacokinetics)</term><term>Lutetium (therapeutic use)</term><term>Mice</term><term>Mice, Nude</term><term>Neoplasm Transplantation</term><term>Neoplasms (radionuclide imaging)</term><term>Neoplasms (radiotherapy)</term><term>Octreotide (diagnostic use)</term><term>Octreotide (metabolism)</term><term>Octreotide (pharmacokinetics)</term><term>Octreotide (therapeutic use)</term><term>Organometallic Compounds (diagnostic use)</term><term>Organometallic Compounds (metabolism)</term><term>Organometallic Compounds (pharmacokinetics)</term><term>Organometallic Compounds (therapeutic use)</term><term>Radiopharmaceuticals (diagnostic use)</term><term>Radiopharmaceuticals (metabolism)</term><term>Radiopharmaceuticals (pharmacokinetics)</term><term>Radiopharmaceuticals (therapeutic use)</term><term>Receptors, Somatostatin (antagonists & inhibitors)</term><term>Receptors, Somatostatin (metabolism)</term><term>Tissue Distribution</term></keywords><keywords scheme="MESH" type="chemical" qualifier="antagonists & inhibitors" xml:lang="en"><term>Receptors, Somatostatin</term></keywords><keywords scheme="MESH" type="chemical" qualifier="diagnostic use" xml:lang="en"><term>Indium Radioisotopes</term><term>Lutetium</term><term>Octreotide</term><term>Organometallic Compounds</term><term>Radiopharmaceuticals</term></keywords><keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Indium Radioisotopes</term><term>Lutetium</term><term>Octreotide</term><term>Organometallic Compounds</term><term>Radiopharmaceuticals</term><term>Receptors, Somatostatin</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacokinetics" xml:lang="en"><term>Indium Radioisotopes</term><term>Lutetium</term><term>Octreotide</term><term>Organometallic Compounds</term><term>Radiopharmaceuticals</term></keywords><keywords scheme="MESH" type="chemical" qualifier="therapeutic use" xml:lang="en"><term>Indium Radioisotopes</term><term>Lutetium</term><term>Octreotide</term><term>Organometallic Compounds</term><term>Radiopharmaceuticals</term></keywords><keywords scheme="MESH" qualifier="radionuclide imaging" xml:lang="en"><term>Neoplasms</term></keywords><keywords scheme="MESH" qualifier="radiotherapy" xml:lang="en"><term>Neoplasms</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Female</term><term>HEK293 Cells</term><term>Humans</term><term>Mice</term><term>Mice, Nude</term><term>Neoplasm Transplantation</term><term>Tissue Distribution</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Targeting of tumours positive for somatostatin receptors (sst) with radiolabelled peptides is of interest for tumour localization, staging, therapy follow-up and targeted radionuclide therapy. The peptides used clinically are exclusively agonists, but recently we have shown that the radiolabelled somatostatin-based antagonist (111)In-DOTA-sst2-ANT may be preferable to agonists. However, a comprehensive study of this radiolabelled antagonist to determine its significance was lacking. The present report describes the evaluation of this novel antagonist labelled with (111)In and (177)Lu in three different tumour models.</div></front></TEI><pubmed><MedlineCitation Owner="NLM" Status="MEDLINE"><PMID Version="1">22926735</PMID><DateCreated><Year>2012</Year><Month>11</Month><Day>09</Day></DateCreated><DateCompleted><Year>2013</Year><Month>05</Month><Day>07</Day></DateCompleted><DateRevised><Year>2013</Year><Month>11</Month><Day>21</Day></DateRevised><Article PubModel="Print-Electronic"><Journal><ISSN IssnType="Electronic">1619-7089</ISSN><JournalIssue CitedMedium="Internet"><Volume>39</Volume><Issue>12</Issue><PubDate><Year>2012</Year><Month>Dec</Month></PubDate></JournalIssue><Title>European journal of nuclear medicine and molecular imaging</Title><ISOAbbreviation>Eur. J. Nucl. Med. Mol. Imaging</ISOAbbreviation></Journal><ArticleTitle>Comprehensive evaluation of a somatostatin-based radiolabelled antagonist for diagnostic imaging and radionuclide therapy.</ArticleTitle><Pagination><MedlinePgn>1876-85</MedlinePgn></Pagination><ELocationID EIdType="doi" ValidYN="Y">10.1007/s00259-012-2231-8</ELocationID><Abstract><AbstractText Label="PURPOSE" NlmCategory="OBJECTIVE">Targeting of tumours positive for somatostatin receptors (sst) with radiolabelled peptides is of interest for tumour localization, staging, therapy follow-up and targeted radionuclide therapy. The peptides used clinically are exclusively agonists, but recently we have shown that the radiolabelled somatostatin-based antagonist (111)In-DOTA-sst2-ANT may be preferable to agonists. However, a comprehensive study of this radiolabelled antagonist to determine its significance was lacking. The present report describes the evaluation of this novel antagonist labelled with (111)In and (177)Lu in three different tumour models.</AbstractText><AbstractText Label="METHODS" NlmCategory="METHODS">Radiopeptide binding, internalization and dissociation studies were performed using cells expressing HEK293-rsst(2). Biodistribution studies were performed in HEK293-rsst(2), HEK293-hsst(2) and HEK293-rsst(3) xenografted mice.</AbstractText><AbstractText Label="RESULTS" NlmCategory="RESULTS">Saturation binding analysis confirmed earlier IC(50) data for (111/nat)In-DOTA-sst2-ANT and showed similar affinity of (177/nat)Lu-DOTA-sst2-ANT for the sst(2). Only low internalization was found in cell culture (6.68 ± 0.06 % at 4 h), which was not unexpected for an antagonist, and this could be further reduced by the addition of sucrose. No internalization was observed in HEK293 cells not expressing sst. Both results indicate that the internalization was specific. (111)In-DOTA-sst2-ANT and (177)Lu-DOTA-sst2-ANT were shown to target tumour xenografts expressing the rat and the human sst(2) receptor with no differences in their uptake or pharmacokinetics. The uptake in rsst(2) and hsst(2) was high (about 30 %IA/g 4 h after injection) and surprisingly long-lasting (about 20-23 %IA/g 24 h after injection). Kidney uptake was blocked by approximately 50 % by lysine or Gelofusine.</AbstractText><AbstractText Label="CONCLUSION" NlmCategory="CONCLUSIONS">These results indicate that radiolabelled somatostatin-based antagonists may be superior to corresponding agonists. The long tumour retention time of (177)Lu-DOTA-sst2-ANT indicates that this new class of compounds is of relevance not only in diagnostic imaging but also in targeted radionuclide therapy of sst-positive tumours.</AbstractText></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Wang</LastName><ForeName>Xuejuan</ForeName><Initials>X</Initials><Affiliation>Division of Radiological Chemistry, University Hospital Basel, Switzerland.</Affiliation></Author><Author ValidYN="Y"><LastName>Fani</LastName><ForeName>Melpomeni</ForeName><Initials>M</Initials></Author><Author ValidYN="Y"><LastName>Schulz</LastName><ForeName>Stefan</ForeName><Initials>S</Initials></Author><Author ValidYN="Y"><LastName>Rivier</LastName><ForeName>Jean</ForeName><Initials>J</Initials></Author><Author ValidYN="Y"><LastName>Reubi</LastName><ForeName>Jean Claude</ForeName><Initials>JC</Initials></Author><Author ValidYN="Y"><LastName>Maecke</LastName><ForeName>Helmut R</ForeName><Initials>HR</Initials></Author></AuthorList><Language>eng</Language><PublicationTypeList><PublicationType>Journal Article</PublicationType><PublicationType>Research Support, Non-U.S. Gov't</PublicationType></PublicationTypeList><ArticleDate DateType="Electronic"><Year>2012</Year><Month>08</Month><Day>29</Day></ArticleDate></Article><MedlineJournalInfo><Country>Germany</Country><MedlineTA>Eur J Nucl Med Mol Imaging</MedlineTA><NlmUniqueID>101140988</NlmUniqueID><ISSNLinking>1619-7070</ISSNLinking></MedlineJournalInfo><ChemicalList><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>111In-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid-Phe(4-NO2)-cyclo(Cys-Tyr-Trp-Lys-Thr-Cys)-Tyr-NH2</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Indium Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Organometallic Compounds</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Radiopharmaceuticals</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Receptors, Somatostatin</NameOfSubstance></Chemical><Chemical><RegistryNumber>5H0DOZ21UJ</RegistryNumber><NameOfSubstance>Lutetium</NameOfSubstance></Chemical><Chemical><RegistryNumber>RWM8CCW8GP</RegistryNumber><NameOfSubstance>Octreotide</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName MajorTopicYN="N">Animals</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Female</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">HEK293 Cells</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Humans</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Indium Radioisotopes</DescriptorName><QualifierName MajorTopicYN="N">diagnostic use</QualifierName><QualifierName MajorTopicYN="N">metabolism</QualifierName><QualifierName MajorTopicYN="N">pharmacokinetics</QualifierName><QualifierName MajorTopicYN="N">therapeutic use</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Lutetium</DescriptorName><QualifierName MajorTopicYN="N">diagnostic use</QualifierName><QualifierName MajorTopicYN="N">metabolism</QualifierName><QualifierName MajorTopicYN="N">pharmacokinetics</QualifierName><QualifierName MajorTopicYN="N">therapeutic use</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice, Nude</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Neoplasm Transplantation</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Neoplasms</DescriptorName><QualifierName MajorTopicYN="N">radionuclide 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