Improving radiopeptide pharmacokinetics by adjusting experimental conditions for bombesin receptor-targeted imaging of prostate cancer.
Identifieur interne : 000C97 ( Main/Exploration ); précédent : 000C96; suivant : 000C98Improving radiopeptide pharmacokinetics by adjusting experimental conditions for bombesin receptor-targeted imaging of prostate cancer.
Auteurs : RBID : pubmed:23069925English descriptors
- KwdEn :
- Animals, Bombesin (analogs & derivatives), Bombesin (diagnostic use), Bombesin (pharmacokinetics), Cell Line, Tumor, Humans, Indium Radioisotopes (diagnostic use), Male, Mice, Mice, Nude, Molecular Targeted Therapy, Neoplasm Transplantation, Oligopeptides (diagnostic use), Prostatic Neoplasms (metabolism), Prostatic Neoplasms (radionuclide imaging), Radiopharmaceuticals (diagnostic use), Radiopharmaceuticals (pharmacokinetics), Receptors, Bombesin (metabolism).
- MESH :
- chemical , analogs & derivatives : Bombesin.
- chemical , diagnostic use : Bombesin, Indium Radioisotopes, Oligopeptides, Radiopharmaceuticals.
- chemical , metabolism : Receptors, Bombesin.
- chemical , pharmacokinetics : Bombesin, Radiopharmaceuticals.
- metabolism : Prostatic Neoplasms.
- radionuclide imaging : Prostatic Neoplasms.
- Animals, Cell Line, Tumor, Humans, Male, Mice, Mice, Nude, Molecular Targeted Therapy, Neoplasm Transplantation.
Abstract
Prostate cancer (PC) is a major health problem. The Gastrin-Releasing Peptide Receptor (GRPR) offers a promising target for staging and monitoring of PC since it is overexpressed in PC and not in normal prostatic tissue. To improve receptor-mediated imaging we investigated the impact of various experimental conditions on pharmacokinetics using the Indium-111 labelled bombesin (BN) analogue AMBA. Besides frequently used androgen-resistant PC-3 also the clinically more relevant androgen sensitive VCaP celline was used as human PC xenograft in nude mice.
PubMed: 23069925
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Improving radiopeptide pharmacokinetics by adjusting experimental conditions for bombesin receptor-targeted imaging of prostate cancer.</title><author><name sortKey="Schroeder, R P J" uniqKey="Schroeder R">R P J Schroeder</name><affiliation wicri:level="1"><nlm:affiliation>Department of Nuclear Medicine, Erasmus MC, Rotterdam, the Netherlands.</nlm:affiliation><country xml:lang="fr" wicri:curation="lc">Pays-Bas</country><wicri:regionArea>Department of Nuclear Medicine, Erasmus MC, Rotterdam</wicri:regionArea></affiliation></author><author><name sortKey="De Blois, E" uniqKey="De Blois E">E De Blois</name></author><author><name sortKey="De Ridder, C M A" uniqKey="De Ridder C">C M A De Ridder</name></author><author><name sortKey="Van Weerden, W M" uniqKey="Van Weerden W">W M Van Weerden</name></author><author><name sortKey="Breeman, W A P" uniqKey="Breeman W">W A P Breeman</name></author><author><name sortKey="De Jong, M" uniqKey="De Jong M">M de Jong</name></author></titleStmt><publicationStmt><date when="2012">2012</date><idno type="RBID">pubmed:23069925</idno><idno type="pmid">23069925</idno><idno type="wicri:Area/Main/Corpus">000985</idno><idno type="wicri:Area/Main/Curation">000985</idno><idno type="wicri:Area/Main/Exploration">000C97</idno></publicationStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Bombesin (analogs & derivatives)</term><term>Bombesin (diagnostic use)</term><term>Bombesin (pharmacokinetics)</term><term>Cell Line, Tumor</term><term>Humans</term><term>Indium Radioisotopes (diagnostic use)</term><term>Male</term><term>Mice</term><term>Mice, Nude</term><term>Molecular Targeted Therapy</term><term>Neoplasm Transplantation</term><term>Oligopeptides (diagnostic use)</term><term>Prostatic Neoplasms (metabolism)</term><term>Prostatic Neoplasms (radionuclide imaging)</term><term>Radiopharmaceuticals (diagnostic use)</term><term>Radiopharmaceuticals (pharmacokinetics)</term><term>Receptors, Bombesin (metabolism)</term></keywords><keywords scheme="MESH" type="chemical" qualifier="analogs & derivatives" xml:lang="en"><term>Bombesin</term></keywords><keywords scheme="MESH" type="chemical" qualifier="diagnostic use" xml:lang="en"><term>Bombesin</term><term>Indium Radioisotopes</term><term>Oligopeptides</term><term>Radiopharmaceuticals</term></keywords><keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Receptors, Bombesin</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacokinetics" xml:lang="en"><term>Bombesin</term><term>Radiopharmaceuticals</term></keywords><keywords scheme="MESH" qualifier="metabolism" xml:lang="en"><term>Prostatic Neoplasms</term></keywords><keywords scheme="MESH" qualifier="radionuclide imaging" xml:lang="en"><term>Prostatic Neoplasms</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Cell Line, Tumor</term><term>Humans</term><term>Male</term><term>Mice</term><term>Mice, Nude</term><term>Molecular Targeted Therapy</term><term>Neoplasm Transplantation</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Prostate cancer (PC) is a major health problem. The Gastrin-Releasing Peptide Receptor (GRPR) offers a promising target for staging and monitoring of PC since it is overexpressed in PC and not in normal prostatic tissue. To improve receptor-mediated imaging we investigated the impact of various experimental conditions on pharmacokinetics using the Indium-111 labelled bombesin (BN) analogue AMBA. Besides frequently used androgen-resistant PC-3 also the clinically more relevant androgen sensitive VCaP celline was used as human PC xenograft in nude mice.</div></front></TEI><pubmed><MedlineCitation Owner="NLM" Status="MEDLINE"><PMID Version="1">23069925</PMID><DateCreated><Year>2012</Year><Month>10</Month><Day>16</Day></DateCreated><DateCompleted><Year>2013</Year><Month>03</Month><Day>01</Day></DateCompleted><DateRevised><Year>2013</Year><Month>11</Month><Day>21</Day></DateRevised><Article PubModel="Print"><Journal><ISSN IssnType="Print">1824-4785</ISSN><JournalIssue CitedMedium="Print"><Volume>56</Volume><Issue>5</Issue><PubDate><Year>2012</Year><Month>Oct</Month></PubDate></JournalIssue><Title>The quarterly journal of nuclear medicine and molecular imaging : official publication of the Italian Association of Nuclear Medicine (AIMN) [and] the International Association of Radiopharmacology (IAR), [and] Section of the Society of Radiopharmaceutical Chemistry and Biology</Title><ISOAbbreviation>Q J Nucl Med Mol Imaging</ISOAbbreviation></Journal><ArticleTitle>Improving radiopeptide pharmacokinetics by adjusting experimental conditions for bombesin receptor-targeted imaging of prostate cancer.</ArticleTitle><Pagination><MedlinePgn>468-75</MedlinePgn></Pagination><Abstract><AbstractText Label="AIM" NlmCategory="OBJECTIVE">Prostate cancer (PC) is a major health problem. The Gastrin-Releasing Peptide Receptor (GRPR) offers a promising target for staging and monitoring of PC since it is overexpressed in PC and not in normal prostatic tissue. To improve receptor-mediated imaging we investigated the impact of various experimental conditions on pharmacokinetics using the Indium-111 labelled bombesin (BN) analogue AMBA. Besides frequently used androgen-resistant PC-3 also the clinically more relevant androgen sensitive VCaP celline was used as human PC xenograft in nude mice.</AbstractText><AbstractText Label="METHODS" NlmCategory="METHODS">Non-purified [111In]AMBA was compared with HPLC-purified [111In]AMBA. Effect of specific activity was studied administering 0.1MBq [111In]AMBA supplemented with different amounts of AMBA (1-3000pmol). GRPR was saturated with Tyr4-BN 1 and 4h prior to injection of [111In]AMBA.</AbstractText><AbstractText Label="RESULTS" NlmCategory="RESULTS">GRPR-positive tissue showed a significant 2 to 3-fold increase in absolute uptake after HPLC-purification while keeping a stable tumor-to-pancreas ratio. Lowering specific activity resulted in decline in uptake to 43% in tumor, 49% in kidney and 92% in pancreas between 10 and 3000 pmol. Tumor-to-pancreas ratio improved six-fold from 0.1±0 after 10 pmol up to 0.6±0.2 after 3000 pmol (P<0.01). When saturating GRPR 4h prior to [111In]AMBA injection tumor-to-pancreas ratio improved from 0.10±0.3 to 0.22±0.2 (P<0.01) and tumor-to-kidney ratio increased from 0.92±0.16 to 3.45±0.5 (P<0.01).</AbstractText><AbstractText Label="CONCLUSION" NlmCategory="CONCLUSIONS">Besides specific peptide characteristics also the experimental conditions, such as HPLC-purification, variations in specific activity and saturation of the GRPR prior to [111In]AMBA administration essentially affect radiopeptide pharmacokinetics. Experimental conditions therefore need to be carefully selected in order to compose ideal standardised protocols for optimal targeting.</AbstractText></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Schroeder</LastName><ForeName>R P J</ForeName><Initials>RP</Initials><Affiliation>Department of Nuclear Medicine, Erasmus MC, Rotterdam, the Netherlands.</Affiliation></Author><Author ValidYN="Y"><LastName>De Blois</LastName><ForeName>E</ForeName><Initials>E</Initials></Author><Author ValidYN="Y"><LastName>De Ridder</LastName><ForeName>C M A</ForeName><Initials>CM</Initials></Author><Author ValidYN="Y"><LastName>Van Weerden</LastName><ForeName>W M</ForeName><Initials>WM</Initials></Author><Author ValidYN="Y"><LastName>Breeman</LastName><ForeName>W A P</ForeName><Initials>WA</Initials></Author><Author ValidYN="Y"><LastName>de Jong</LastName><ForeName>M</ForeName><Initials>M</Initials></Author></AuthorList><Language>eng</Language><PublicationTypeList><PublicationType>Journal Article</PublicationType><PublicationType>Research Support, Non-U.S. Gov't</PublicationType></PublicationTypeList></Article><MedlineJournalInfo><Country>Italy</Country><MedlineTA>Q J Nucl Med Mol Imaging</MedlineTA><NlmUniqueID>101213861</NlmUniqueID><ISSNLinking>1824-4785</ISSNLinking></MedlineJournalInfo><ChemicalList><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>DO3A-CH2CO-G-4-aminobenzoyl-Q-W-A-V-G-H-L-M-NH2</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Indium Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Oligopeptides</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Radiopharmaceuticals</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Receptors, Bombesin</NameOfSubstance></Chemical><Chemical><RegistryNumber>PX9AZU7QPK</RegistryNumber><NameOfSubstance>Bombesin</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName MajorTopicYN="N">Animals</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Bombesin</DescriptorName><QualifierName MajorTopicYN="Y">analogs & derivatives</QualifierName><QualifierName MajorTopicYN="Y">diagnostic use</QualifierName><QualifierName MajorTopicYN="N">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Cell Line, Tumor</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Humans</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Indium Radioisotopes</DescriptorName><QualifierName MajorTopicYN="Y">diagnostic use</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Male</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice, Nude</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Molecular Targeted Therapy</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Neoplasm Transplantation</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Oligopeptides</DescriptorName><QualifierName MajorTopicYN="Y">diagnostic use</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Prostatic Neoplasms</DescriptorName><QualifierName MajorTopicYN="N">metabolism</QualifierName><QualifierName MajorTopicYN="Y">radionuclide imaging</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Radiopharmaceuticals</DescriptorName><QualifierName MajorTopicYN="Y">diagnostic use</QualifierName><QualifierName MajorTopicYN="N">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Receptors, Bombesin</DescriptorName><QualifierName MajorTopicYN="Y">metabolism</QualifierName></MeshHeading></MeshHeadingList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="entrez"><Year>2012</Year><Month>10</Month><Day>17</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="pubmed"><Year>2012</Year><Month>10</Month><Day>17</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>2013</Year><Month>3</Month><Day>2</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId IdType="pii">R39122414</ArticleId><ArticleId IdType="pubmed">23069925</ArticleId></ArticleIdList></PubmedData></pubmed></record>Pour manipuler ce document sous Unix (Dilib)
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