Exendin-4-based radiopharmaceuticals for glucagonlike peptide-1 receptor PET/CT and SPECT/CT.
Identifieur interne : 001989 ( Main/Exploration ); précédent : 001988; suivant : 001990Exendin-4-based radiopharmaceuticals for glucagonlike peptide-1 receptor PET/CT and SPECT/CT.
Auteurs : RBID : pubmed:20595511English descriptors
- KwdEn :
- Animals, Cells, Cultured, Dose-Response Relationship, Radiation, Female, Gallium Radioisotopes (diagnostic use), Indicators and Reagents, Indium Radioisotopes (diagnostic use), Isotope Labeling, Kidney (metabolism), Kidney (radionuclide imaging), Male, Mice, Mice, Transgenic, Peptides (chemistry), Peptides (diagnostic use), Positron-Emission Tomography, Radiopharmaceuticals (chemistry), Radiopharmaceuticals (diagnostic use), Receptors, Glucagon (metabolism), Technetium Compounds (diagnostic use), Tissue Distribution, Tomography, Emission-Computed, Tomography, Emission-Computed, Single-Photon, Venoms (chemistry), Venoms (diagnostic use).
- MESH :
- chemical , chemistry : Peptides, Radiopharmaceuticals, Venoms.
- chemical , diagnostic use : Gallium Radioisotopes, Indium Radioisotopes, Peptides, Radiopharmaceuticals, Technetium Compounds, Venoms.
- metabolism : Kidney, Receptors, Glucagon.
- radionuclide imaging : Kidney.
- Animals, Cells, Cultured, Dose-Response Relationship, Radiation, Female, Indicators and Reagents, Isotope Labeling, Male, Mice, Mice, Transgenic, Positron-Emission Tomography, Tissue Distribution, Tomography, Emission-Computed, Tomography, Emission-Computed, Single-Photon.
Abstract
Strong overexpression of glucagonlike peptide-1 (GLP-1) receptors in human insulinoma provides an attractive target for imaging. The first clinical trials demonstrated that GLP-1 receptor SPECT/CT using [Lys(40)(Ahx [6-aminohexanoic acid]-DOTA-(111)In)NH(2)]-exendin-4 can localize hardly detectable insulinomas. However, [Lys(40)(Ahx-DOTA-(111)In)NH(2)]-exendin-4 imaging has drawbacks related to the use of (111)In in that it is costly and carries a relatively high radiation burden for the patient. The aim of this study was the preclinical evaluation of [Lys(40)(Ahx-DOTA-(68)Ga)NH(2)]-exendin-4 for PET/CT and [Lys(40)(Ahx-hydrazinonicotinamide [HYNIC]-(99m)Tc)NH(2)]-exendin-4 for SPECT/CT.
DOI: 10.2967/jnumed.110.074914
PubMed: 20595511
Links toward previous steps (curation, corpus...)
Le document en format XML
<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Exendin-4-based radiopharmaceuticals for glucagonlike peptide-1 receptor PET/CT and SPECT/CT.</title><author><name sortKey="Wild, Damian" uniqKey="Wild D">Damian Wild</name><affiliation wicri:level="1"><nlm:affiliation>Clinic and Institute of Nuclear Medicine, University Hospital Basel, Basel, Switzerland.</nlm:affiliation><country xml:lang="fr">Suisse</country><wicri:regionArea>Clinic and Institute of Nuclear Medicine, University Hospital Basel, Basel</wicri:regionArea></affiliation></author><author><name sortKey="Wicki, Andreas" uniqKey="Wicki A">Andreas Wicki</name></author><author><name sortKey="Mansi, Rosalba" uniqKey="Mansi R">Rosalba Mansi</name></author><author><name sortKey="Behe, Martin" uniqKey="Behe M">Martin Béhé</name></author><author><name sortKey="Keil, Boris" uniqKey="Keil B">Boris Keil</name></author><author><name sortKey="Bernhardt, Peter" uniqKey="Bernhardt P">Peter Bernhardt</name></author><author><name sortKey="Christofori, Gerhard" uniqKey="Christofori G">Gerhard Christofori</name></author><author><name sortKey="Ell, Peter J" uniqKey="Ell P">Peter J Ell</name></author><author><name sortKey="M Cke, Helmut R" uniqKey="M Cke H">Helmut R Mäcke</name></author></titleStmt><publicationStmt><date when="2010">2010</date><idno type="doi">10.2967/jnumed.110.074914</idno><idno type="RBID">pubmed:20595511</idno><idno type="pmid">20595511</idno><idno type="wicri:Area/Main/Corpus">001868</idno><idno type="wicri:Area/Main/Curation">001868</idno><idno type="wicri:Area/Main/Exploration">001989</idno></publicationStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Cells, Cultured</term><term>Dose-Response Relationship, Radiation</term><term>Female</term><term>Gallium Radioisotopes (diagnostic use)</term><term>Indicators and Reagents</term><term>Indium Radioisotopes (diagnostic use)</term><term>Isotope Labeling</term><term>Kidney (metabolism)</term><term>Kidney (radionuclide imaging)</term><term>Male</term><term>Mice</term><term>Mice, Transgenic</term><term>Peptides (chemistry)</term><term>Peptides (diagnostic use)</term><term>Positron-Emission Tomography</term><term>Radiopharmaceuticals (chemistry)</term><term>Radiopharmaceuticals (diagnostic use)</term><term>Receptors, Glucagon (metabolism)</term><term>Technetium Compounds (diagnostic use)</term><term>Tissue Distribution</term><term>Tomography, Emission-Computed</term><term>Tomography, Emission-Computed, Single-Photon</term><term>Venoms (chemistry)</term><term>Venoms (diagnostic use)</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Peptides</term><term>Radiopharmaceuticals</term><term>Venoms</term></keywords><keywords scheme="MESH" type="chemical" qualifier="diagnostic use" xml:lang="en"><term>Gallium Radioisotopes</term><term>Indium Radioisotopes</term><term>Peptides</term><term>Radiopharmaceuticals</term><term>Technetium Compounds</term><term>Venoms</term></keywords><keywords scheme="MESH" qualifier="metabolism" xml:lang="en"><term>Kidney</term><term>Receptors, Glucagon</term></keywords><keywords scheme="MESH" qualifier="radionuclide imaging" xml:lang="en"><term>Kidney</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Cells, Cultured</term><term>Dose-Response Relationship, Radiation</term><term>Female</term><term>Indicators and Reagents</term><term>Isotope Labeling</term><term>Male</term><term>Mice</term><term>Mice, Transgenic</term><term>Positron-Emission Tomography</term><term>Tissue Distribution</term><term>Tomography, Emission-Computed</term><term>Tomography, Emission-Computed, Single-Photon</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Strong overexpression of glucagonlike peptide-1 (GLP-1) receptors in human insulinoma provides an attractive target for imaging. The first clinical trials demonstrated that GLP-1 receptor SPECT/CT using [Lys(40)(Ahx [6-aminohexanoic acid]-DOTA-(111)In)NH(2)]-exendin-4 can localize hardly detectable insulinomas. However, [Lys(40)(Ahx-DOTA-(111)In)NH(2)]-exendin-4 imaging has drawbacks related to the use of (111)In in that it is costly and carries a relatively high radiation burden for the patient. The aim of this study was the preclinical evaluation of [Lys(40)(Ahx-DOTA-(68)Ga)NH(2)]-exendin-4 for PET/CT and [Lys(40)(Ahx-hydrazinonicotinamide [HYNIC]-(99m)Tc)NH(2)]-exendin-4 for SPECT/CT.</div></front></TEI><pubmed><MedlineCitation Owner="NLM" Status="MEDLINE"><PMID Version="1">20595511</PMID><DateCreated><Year>2010</Year><Month>07</Month><Day>02</Day></DateCreated><DateCompleted><Year>2010</Year><Month>07</Month><Day>27</Day></DateCompleted><DateRevised><Year>2013</Year><Month>11</Month><Day>21</Day></DateRevised><Article PubModel="Print"><Journal><ISSN IssnType="Electronic">1535-5667</ISSN><JournalIssue CitedMedium="Internet"><Volume>51</Volume><Issue>7</Issue><PubDate><Year>2010</Year><Month>Jul</Month></PubDate></JournalIssue><Title>Journal of nuclear medicine : official publication, Society of Nuclear Medicine</Title><ISOAbbreviation>J. Nucl. Med.</ISOAbbreviation></Journal><ArticleTitle>Exendin-4-based radiopharmaceuticals for glucagonlike peptide-1 receptor PET/CT and SPECT/CT.</ArticleTitle><Pagination><MedlinePgn>1059-67</MedlinePgn></Pagination><ELocationID EIdType="doi" ValidYN="Y">10.2967/jnumed.110.074914</ELocationID><Abstract><AbstractText Label="UNLABELLED">Strong overexpression of glucagonlike peptide-1 (GLP-1) receptors in human insulinoma provides an attractive target for imaging. The first clinical trials demonstrated that GLP-1 receptor SPECT/CT using [Lys(40)(Ahx [6-aminohexanoic acid]-DOTA-(111)In)NH(2)]-exendin-4 can localize hardly detectable insulinomas. However, [Lys(40)(Ahx-DOTA-(111)In)NH(2)]-exendin-4 imaging has drawbacks related to the use of (111)In in that it is costly and carries a relatively high radiation burden for the patient. The aim of this study was the preclinical evaluation of [Lys(40)(Ahx-DOTA-(68)Ga)NH(2)]-exendin-4 for PET/CT and [Lys(40)(Ahx-hydrazinonicotinamide [HYNIC]-(99m)Tc)NH(2)]-exendin-4 for SPECT/CT.</AbstractText><AbstractText Label="METHODS" NlmCategory="METHODS">Internalization, biodistribution, dosimetry, and imaging studies were performed in the Rip1Tag2 mouse model of pancreatic beta-cell carcinogenesis and compared with our gold standard [Lys(40)(Ahx-DOTA-(111)In)NH(2)]-exendin-4. Poly-glutamic acid and Gelofusine, a gelatin-based plasma expander, were used for renal uptake reduction studies.</AbstractText><AbstractText Label="RESULTS" NlmCategory="RESULTS">The tumor uptake of [Lys(40)(Ahx-DOTA-(68)Ga)NH(2)]-exendin-4 was 205 +/- 59 percentage injected activity per gram of tissue at 4 h. Other GLP-1 receptor-positive organs showed more than 4.8 times lower radioactivity uptake. [Lys(40)(Ahx-HYNIC-(99m)Tc/ethylenediaminediacetic acid [EDDA])NH(2)]-exendin-4, compared with its (111)In- and (68)Ga-labeled sister compounds, showed significantly less tumor and organ uptake. The significantly lower tumor and organ uptake of [Lys(40)(Ahx-HYNIC-(99m)Tc/EDDA)NH(2)]-exendin-4 did not result in inferior tumor-to-organ ratios or reduced image quality. All radiopeptides tested showed a high tumor-to-background ratio, resulting in the visualization of small tumors (maximum diameter between 1.0 and 3.2 mm) by SPECT and PET. The only exception was the kidneys, which also showed high uptake. This uptake could be reduced by 49%-78% using poly-glutamic acid, Gelofusine, or a combination of the 2. The estimated effective radiation dose was 3.7 muSv/MBq for [Lys(40)(Ahx-HYNIC-(99m)Tc/EDDA)NH(2)]-exendin-4, which was 8 times less than that for [Lys(40)(Ahx-DOTA-(68)Ga)NH(2)]-exendin-4 and 43 times less than that for [Lys(40)(Ahx-DOTA-(111)In)NH(2)]-exendin-4.</AbstractText><AbstractText Label="CONCLUSION" NlmCategory="CONCLUSIONS">These promising pharmacokinetic and imaging data show that [Lys(40)(Ahx-DOTA-(68)Ga)NH(2)]-exendin-4 and [Lys(40)(Ahx-HYNIC-(99m)Tc/EDDA)NH(2)]-exendin-4 are suitable candidates for clinical GLP-1 receptor imaging studies.</AbstractText></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Wild</LastName><ForeName>Damian</ForeName><Initials>D</Initials><Affiliation>Clinic and Institute of Nuclear Medicine, University Hospital Basel, Basel, Switzerland.</Affiliation></Author><Author ValidYN="Y"><LastName>Wicki</LastName><ForeName>Andreas</ForeName><Initials>A</Initials></Author><Author ValidYN="Y"><LastName>Mansi</LastName><ForeName>Rosalba</ForeName><Initials>R</Initials></Author><Author ValidYN="Y"><LastName>Béhé</LastName><ForeName>Martin</ForeName><Initials>M</Initials></Author><Author ValidYN="Y"><LastName>Keil</LastName><ForeName>Boris</ForeName><Initials>B</Initials></Author><Author ValidYN="Y"><LastName>Bernhardt</LastName><ForeName>Peter</ForeName><Initials>P</Initials></Author><Author ValidYN="Y"><LastName>Christofori</LastName><ForeName>Gerhard</ForeName><Initials>G</Initials></Author><Author ValidYN="Y"><LastName>Ell</LastName><ForeName>Peter J</ForeName><Initials>PJ</Initials></Author><Author ValidYN="Y"><LastName>Mäcke</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></Article><MedlineJournalInfo><Country>United States</Country><MedlineTA>J Nucl Med</MedlineTA><NlmUniqueID>0217410</NlmUniqueID><ISSNLinking>0161-5505</ISSNLinking></MedlineJournalInfo><ChemicalList><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Gallium Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Indicators and Reagents</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Indium Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Peptides</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Radiopharmaceuticals</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Receptors, Glucagon</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Technetium Compounds</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Venoms</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>glucagon-like peptide-1 receptor</NameOfSubstance></Chemical><Chemical><RegistryNumber>9P1872D4OL</RegistryNumber><NameOfSubstance>exenatide</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName MajorTopicYN="N">Animals</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Cells, Cultured</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Dose-Response Relationship, Radiation</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Female</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Gallium Radioisotopes</DescriptorName><QualifierName MajorTopicYN="N">diagnostic use</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Indicators and Reagents</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Indium Radioisotopes</DescriptorName><QualifierName MajorTopicYN="N">diagnostic use</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Isotope Labeling</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Kidney</DescriptorName><QualifierName MajorTopicYN="N">metabolism</QualifierName><QualifierName MajorTopicYN="N">radionuclide imaging</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Male</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice, Transgenic</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Peptides</DescriptorName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="Y">diagnostic use</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Positron-Emission Tomography</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Radiopharmaceuticals</DescriptorName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="Y">diagnostic use</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Receptors, Glucagon</DescriptorName><QualifierName MajorTopicYN="Y">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Technetium Compounds</DescriptorName><QualifierName MajorTopicYN="N">diagnostic use</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Tissue Distribution</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Tomography, Emission-Computed</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Tomography, Emission-Computed, Single-Photon</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Venoms</DescriptorName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="Y">diagnostic use</QualifierName></MeshHeading></MeshHeadingList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="entrez"><Year>2010</Year><Month>7</Month><Day>3</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="pubmed"><Year>2010</Year><Month>7</Month><Day>3</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>2010</Year><Month>7</Month><Day>28</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId IdType="pii">51/7/1059</ArticleId><ArticleId IdType="doi">10.2967/jnumed.110.074914</ArticleId><ArticleId IdType="pubmed">20595511</ArticleId></ArticleIdList></PubmedData></pubmed></record>Pour manipuler ce document sous Unix (Dilib)
EXPLOR_STEP=IndiumV2/Data/Main/Exploration
HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 001989 | SxmlIndent | more
Ou
HfdSelect -h $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd -nk 001989 | SxmlIndent | more
Pour mettre un lien sur cette page dans le réseau Wicri
{{Explor lien
|wiki= *** parameter Area/wikiCode missing ***
|area= IndiumV2
|flux= Main
|étape= Exploration
|type= RBID
|clé= pubmed:20595511
|texte= Exendin-4-based radiopharmaceuticals for glucagonlike peptide-1 receptor PET/CT and SPECT/CT.
}}
Pour générer des pages wiki
HfdIndexSelect -h $EXPLOR_AREA/Data/Main/Exploration/RBID.i -Sk "pubmed:20595511" \
| HfdSelect -Kh $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd \
| NlmPubMed2Wicri -a IndiumV2
| This area was generated with Dilib version V0.5.76. |  |