Radiosynthesis of 68Ga-labelled DOTA-biocytin (68Ga-r-BHD) and assessment of its pharmaceutical quality for clinical use.
Identifieur interne : 000B12 ( Main/Exploration ); précédent : 000B11; suivant : 000B13Radiosynthesis of 68Ga-labelled DOTA-biocytin (68Ga-r-BHD) and assessment of its pharmaceutical quality for clinical use.
Auteurs : RBID : pubmed:22836735English descriptors
- KwdEn :
- Avidin (metabolism), Clinical Trials as Topic, Drug Stability, Gallium Radioisotopes (chemistry), Heterocyclic Compounds, 1-Ring (chemistry), Humans, Lysine (analogs & derivatives), Lysine (blood), Lysine (chemistry), Lysine (diagnostic use), Lysine (metabolism), Quality Control, Radiochemistry (methods), Safety.
- MESH :
- chemical , analogs & derivatives : Lysine.
- chemical , blood : Lysine.
- chemical , chemistry : Gallium Radioisotopes, Heterocyclic Compounds, 1-Ring, Lysine.
- chemical , diagnostic use : Lysine.
- chemical , metabolism : Avidin, Lysine.
- methods : Radiochemistry.
- Clinical Trials as Topic, Drug Stability, Humans, Quality Control, Safety.
Abstract
Biocytin analogues labelled with indium-111, yttrium-90 and lutetium-177 have shown their effectiveness in the imaging of infections/inflammation in patients with osteomyelitis and function as efficient tools in pretargeted antibody-guided radioimmunotherapy. In this study, the labelling of a biocytin analogue coupled with DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), namely, r-BHD, with gallium-68 (68Ga) was optimized, and the quality and stability of the preparations were assessed for clinical use.
DOI: 10.1097/MNM.0b013e3283573e05
PubMed: 22836735
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Radiosynthesis of 68Ga-labelled DOTA-biocytin (68Ga-r-BHD) and assessment of its pharmaceutical quality for clinical use.</title><author><name sortKey="Asti, Mattia" uniqKey="Asti M">Mattia Asti</name><affiliation wicri:level="1"><nlm:affiliation>Nuclear Medicine Unit, Advanced Technology Department, Santa Maria Nuova Hospital-IRCCS, Reggio Emilia, Italy. asti.mattia@asmn.re.it</nlm:affiliation><country xml:lang="fr">Italie</country><wicri:regionArea>Nuclear Medicine Unit, Advanced Technology Department, Santa Maria Nuova Hospital-IRCCS, Reggio Emilia</wicri:regionArea></affiliation></author><author><name sortKey="Iori, Michele" uniqKey="Iori M">Michele Iori</name></author><author><name sortKey="Erba, Paola A" uniqKey="Erba P">Paola A Erba</name></author><author><name sortKey="Atti, Giulia" uniqKey="Atti G">Giulia Atti</name></author><author><name sortKey="Farioli, Daniela" uniqKey="Farioli D">Daniela Farioli</name></author><author><name sortKey="Guidotti, Claudio" uniqKey="Guidotti C">Claudio Guidotti</name></author><author><name sortKey="Versari, Annibale" uniqKey="Versari A">Annibale Versari</name></author></titleStmt><publicationStmt><date when="2012">2012</date><idno type="doi">10.1097/MNM.0b013e3283573e05</idno><idno type="RBID">pubmed:22836735</idno><idno type="pmid">22836735</idno><idno type="wicri:Area/Main/Corpus">000B63</idno><idno type="wicri:Area/Main/Curation">000B63</idno><idno type="wicri:Area/Main/Exploration">000B12</idno></publicationStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Avidin (metabolism)</term><term>Clinical Trials as Topic</term><term>Drug Stability</term><term>Gallium Radioisotopes (chemistry)</term><term>Heterocyclic Compounds, 1-Ring (chemistry)</term><term>Humans</term><term>Lysine (analogs & derivatives)</term><term>Lysine (blood)</term><term>Lysine (chemistry)</term><term>Lysine (diagnostic use)</term><term>Lysine (metabolism)</term><term>Quality Control</term><term>Radiochemistry (methods)</term><term>Safety</term></keywords><keywords scheme="MESH" type="chemical" qualifier="analogs & derivatives" xml:lang="en"><term>Lysine</term></keywords><keywords scheme="MESH" type="chemical" qualifier="blood" xml:lang="en"><term>Lysine</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Gallium Radioisotopes</term><term>Heterocyclic Compounds, 1-Ring</term><term>Lysine</term></keywords><keywords scheme="MESH" type="chemical" qualifier="diagnostic use" xml:lang="en"><term>Lysine</term></keywords><keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Avidin</term><term>Lysine</term></keywords><keywords scheme="MESH" qualifier="methods" xml:lang="en"><term>Radiochemistry</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Clinical Trials as Topic</term><term>Drug Stability</term><term>Humans</term><term>Quality Control</term><term>Safety</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Biocytin analogues labelled with indium-111, yttrium-90 and lutetium-177 have shown their effectiveness in the imaging of infections/inflammation in patients with osteomyelitis and function as efficient tools in pretargeted antibody-guided radioimmunotherapy. In this study, the labelling of a biocytin analogue coupled with DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), namely, r-BHD, with gallium-68 (68Ga) was optimized, and the quality and stability of the preparations were assessed for clinical use.</div></front></TEI><pubmed><MedlineCitation Owner="NLM" Status="MEDLINE"><PMID Version="1">22836735</PMID><DateCreated><Year>2012</Year><Month>09</Month><Day>21</Day></DateCreated><DateCompleted><Year>2013</Year><Month>02</Month><Day>01</Day></DateCompleted><DateRevised><Year>2013</Year><Month>11</Month><Day>21</Day></DateRevised><Article PubModel="Print"><Journal><ISSN IssnType="Electronic">1473-5628</ISSN><JournalIssue CitedMedium="Internet"><Volume>33</Volume><Issue>11</Issue><PubDate><Year>2012</Year><Month>Nov</Month></PubDate></JournalIssue><Title>Nuclear medicine communications</Title><ISOAbbreviation>Nucl Med Commun</ISOAbbreviation></Journal><ArticleTitle>Radiosynthesis of 68Ga-labelled DOTA-biocytin (68Ga-r-BHD) and assessment of its pharmaceutical quality for clinical use.</ArticleTitle><Pagination><MedlinePgn>1179-87</MedlinePgn></Pagination><Abstract><AbstractText Label="OBJECTIVES" NlmCategory="OBJECTIVE">Biocytin analogues labelled with indium-111, yttrium-90 and lutetium-177 have shown their effectiveness in the imaging of infections/inflammation in patients with osteomyelitis and function as efficient tools in pretargeted antibody-guided radioimmunotherapy. In this study, the labelling of a biocytin analogue coupled with DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), namely, r-BHD, with gallium-68 (68Ga) was optimized, and the quality and stability of the preparations were assessed for clinical use.</AbstractText><AbstractText Label="MATERIALS AND METHODS" NlmCategory="METHODS">Synthesis of 68Ga-r-BHD was carried out by heating a fraction of the 68Ge/68Ga eluate in a reactor containing the biocytin analogue with the appropriate buffer. The influence of the precursor amount (from 2.5 to 140 nmol), the pH of the reaction (from 2 to 5.5) and the buffer species (1.5 mol/l sodium acetate, 1.5 mol/l sodium formate, 4.5 mol/l HEPES) on radiochemical yield and radiochemical purity was assessed. Studies on stability and binding to avidin (Av) were also conducted in different media.</AbstractText><AbstractText Label="RESULTS" NlmCategory="RESULTS">Under the best labelling condition (56 nmol of precursor, 3.8 pH, sodium formate buffer) synthesis of 68Ga-r-BHD resulted in a yield of 64 ± 3% (not decay corrected). Radiochemical purity was around 95% because a 68Ga-coordinated sulfoxide form of the ligand was detected as a by-product of the reaction (68Ga-r-SBHD). The by-product was identified and characterized by liquid chromatography-electrospray ionization tandem mass spectrometry. At the natural 1 : 4 Av/68Ga-r-BHD molar ratio, affinity results were 62 ± 2 and 80 ± 2% in saline and human serum, respectively. Stability of 68Ga-r-BHD and of the radiotracer/Av complex remains almost constant over 180 min. 68Ga-r-BHD appears to be a good candidate for clinical applications.</AbstractText></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Asti</LastName><ForeName>Mattia</ForeName><Initials>M</Initials><Affiliation>Nuclear Medicine Unit, Advanced Technology Department, Santa Maria Nuova Hospital-IRCCS, Reggio Emilia, Italy. asti.mattia@asmn.re.it</Affiliation></Author><Author ValidYN="Y"><LastName>Iori</LastName><ForeName>Michele</ForeName><Initials>M</Initials></Author><Author ValidYN="Y"><LastName>Erba</LastName><ForeName>Paola A</ForeName><Initials>PA</Initials></Author><Author ValidYN="Y"><LastName>Atti</LastName><ForeName>Giulia</ForeName><Initials>G</Initials></Author><Author ValidYN="Y"><LastName>Farioli</LastName><ForeName>Daniela</ForeName><Initials>D</Initials></Author><Author ValidYN="Y"><LastName>Guidotti</LastName><ForeName>Claudio</ForeName><Initials>C</Initials></Author><Author ValidYN="Y"><LastName>Versari</LastName><ForeName>Annibale</ForeName><Initials>A</Initials></Author></AuthorList><Language>eng</Language><PublicationTypeList><PublicationType>Journal Article</PublicationType></PublicationTypeList></Article><MedlineJournalInfo><Country>England</Country><MedlineTA>Nucl Med Commun</MedlineTA><NlmUniqueID>8201017</NlmUniqueID><ISSNLinking>0143-3636</ISSNLinking></MedlineJournalInfo><ChemicalList><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Gallium Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Heterocyclic Compounds, 1-Ring</NameOfSubstance></Chemical><Chemical><RegistryNumber>1405-69-2</RegistryNumber><NameOfSubstance>Avidin</NameOfSubstance></Chemical><Chemical><RegistryNumber>60239-18-1</RegistryNumber><NameOfSubstance>1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid</NameOfSubstance></Chemical><Chemical><RegistryNumber>G6D6147J22</RegistryNumber><NameOfSubstance>biocytin</NameOfSubstance></Chemical><Chemical><RegistryNumber>K3Z4F929H6</RegistryNumber><NameOfSubstance>Lysine</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName MajorTopicYN="N">Avidin</DescriptorName><QualifierName MajorTopicYN="N">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Clinical Trials as Topic</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Drug Stability</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Gallium Radioisotopes</DescriptorName><QualifierName MajorTopicYN="N">chemistry</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Heterocyclic Compounds, 1-Ring</DescriptorName><QualifierName MajorTopicYN="Y">chemistry</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Humans</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Lysine</DescriptorName><QualifierName MajorTopicYN="Y">analogs & derivatives</QualifierName><QualifierName MajorTopicYN="N">blood</QualifierName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="N">diagnostic use</QualifierName><QualifierName MajorTopicYN="N">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Quality Control</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Radiochemistry</DescriptorName><QualifierName MajorTopicYN="Y">methods</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Safety</DescriptorName></MeshHeading></MeshHeadingList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="entrez"><Year>2012</Year><Month>7</Month><Day>28</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="pubmed"><Year>2012</Year><Month>7</Month><Day>28</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>2013</Year><Month>2</Month><Day>5</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId IdType="doi">10.1097/MNM.0b013e3283573e05</ArticleId><ArticleId IdType="pubmed">22836735</ArticleId></ArticleIdList></PubmedData></pubmed></record>Pour manipuler ce document sous Unix (Dilib)
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