Radiolabeling, stability studies, and pharmacokinetic evaluation of thulium-170-labeled acyclic and cyclic polyaminopolyphosphonic acids.
Identifieur interne : 000257 ( PubMed/Corpus ); précédent : 000256; suivant : 000258Radiolabeling, stability studies, and pharmacokinetic evaluation of thulium-170-labeled acyclic and cyclic polyaminopolyphosphonic acids.
Auteurs : Kusum Vats ; Tapas Das ; Haladhar D. Sarma ; Sharmila Banerjee ; M R A. PillaiSource :
- Cancer biotherapy & radiopharmaceuticals [ 1557-8852 ] ; 2013.
English descriptors
- KwdEn :
- Animals, Bone and Bones (metabolism), Bone and Bones (pathology), Bone and Bones (radionuclide imaging), Isotope Labeling, Palliative Care, Phosphorous Acids (chemistry), Phosphorous Acids (pharmacokinetics), Polyamines (chemistry), Polyamines (pharmacokinetics), Radioisotopes (chemistry), Radioisotopes (pharmacokinetics), Radiopharmaceuticals (chemistry), Radiopharmaceuticals (pharmacokinetics), Rats, Rats, Wistar, Thulium (chemistry), Thulium (pharmacokinetics), Tissue Distribution.
- MESH :
- chemical , chemistry : Phosphorous Acids, Polyamines, Radioisotopes, Radiopharmaceuticals, Thulium.
- metabolism : Bone and Bones.
- pathology : Bone and Bones.
- chemical , pharmacokinetics : Phosphorous Acids, Polyamines, Radioisotopes, Radiopharmaceuticals, Thulium.
- radionuclide imaging : Bone and Bones.
- Animals, Isotope Labeling, Palliative Care, Rats, Rats, Wistar, Tissue Distribution.
Abstract
Thulium-170 [T1/2=128.4 days, Eβ(max)=968 keV, and Eγ=84 keV (3.26%)] could be considered an easily producible and cost-effective alternative to (89)Sr for the preparation of radiopharmaceuticals for palliation of bone pain arising due to skeletal metastases. Multidentate aminomethylene polyphosphonic acids have already been proven to be effective as carrier moieties for developing radiolabeled bone pain palliation agents using lanthanide radionuclides. Therefore, an attempt was made to evaluate the potential of a series of (170)Tm-labeled acyclic (diethylenetriaminepentamethylene phosphonic acid and triethylenetetraminehexamethylene phosphonic acid) and cyclic polyaminopolyphosphonic acids (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetramethylene phosphonic acid [DOTMP] and 1,4,8,11-tetraazacyclotetradecane-1,4,8,11-tetramethylene phosphonic acid [CTMP]) toward their use as alternative bone pain palliation agents.
DOI: 10.1089/cbr.2013.1475
PubMed: 23931111
Links to Exploration step
pubmed:23931111Le document en format XML
<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Radiolabeling, stability studies, and pharmacokinetic evaluation of thulium-170-labeled acyclic and cyclic polyaminopolyphosphonic acids.</title><author><name sortKey="Vats, Kusum" sort="Vats, Kusum" uniqKey="Vats K" first="Kusum" last="Vats">Kusum Vats</name><affiliation><nlm:affiliation>1 Radiopharmaceuticals Division, Bhabha Atomic Research Centre , Mumbai, India .</nlm:affiliation></affiliation></author><author><name sortKey="Das, Tapas" sort="Das, Tapas" uniqKey="Das T" first="Tapas" last="Das">Tapas Das</name></author><author><name sortKey="Sarma, Haladhar D" sort="Sarma, Haladhar D" uniqKey="Sarma H" first="Haladhar D" last="Sarma">Haladhar D. Sarma</name></author><author><name sortKey="Banerjee, Sharmila" sort="Banerjee, Sharmila" uniqKey="Banerjee S" first="Sharmila" last="Banerjee">Sharmila Banerjee</name></author><author><name sortKey="Pillai, M R A" sort="Pillai, M R A" uniqKey="Pillai M" first="M R A" last="Pillai">M R A. Pillai</name></author></titleStmt><publicationStmt><idno type="wicri:source">PubMed</idno><date when="2013">2013</date><idno type="doi">10.1089/cbr.2013.1475</idno><idno type="RBID">pubmed:23931111</idno><idno type="pmid">23931111</idno><idno type="wicri:Area/PubMed/Corpus">000257</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Corpus" wicri:corpus="PubMed">000257</idno></publicationStmt><sourceDesc><biblStruct><analytic><title xml:lang="en">Radiolabeling, stability studies, and pharmacokinetic evaluation of thulium-170-labeled acyclic and cyclic polyaminopolyphosphonic acids.</title><author><name sortKey="Vats, Kusum" sort="Vats, Kusum" uniqKey="Vats K" first="Kusum" last="Vats">Kusum Vats</name><affiliation><nlm:affiliation>1 Radiopharmaceuticals Division, Bhabha Atomic Research Centre , Mumbai, India .</nlm:affiliation></affiliation></author><author><name sortKey="Das, Tapas" sort="Das, Tapas" uniqKey="Das T" first="Tapas" last="Das">Tapas Das</name></author><author><name sortKey="Sarma, Haladhar D" sort="Sarma, Haladhar D" uniqKey="Sarma H" first="Haladhar D" last="Sarma">Haladhar D. Sarma</name></author><author><name sortKey="Banerjee, Sharmila" sort="Banerjee, Sharmila" uniqKey="Banerjee S" first="Sharmila" last="Banerjee">Sharmila Banerjee</name></author><author><name sortKey="Pillai, M R A" sort="Pillai, M R A" uniqKey="Pillai M" first="M R A" last="Pillai">M R A. Pillai</name></author></analytic><series><title level="j">Cancer biotherapy & radiopharmaceuticals</title><idno type="eISSN">1557-8852</idno><imprint><date when="2013" type="published">2013</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Bone and Bones (metabolism)</term><term>Bone and Bones (pathology)</term><term>Bone and Bones (radionuclide imaging)</term><term>Isotope Labeling</term><term>Palliative Care</term><term>Phosphorous Acids (chemistry)</term><term>Phosphorous Acids (pharmacokinetics)</term><term>Polyamines (chemistry)</term><term>Polyamines (pharmacokinetics)</term><term>Radioisotopes (chemistry)</term><term>Radioisotopes (pharmacokinetics)</term><term>Radiopharmaceuticals (chemistry)</term><term>Radiopharmaceuticals (pharmacokinetics)</term><term>Rats</term><term>Rats, Wistar</term><term>Thulium (chemistry)</term><term>Thulium (pharmacokinetics)</term><term>Tissue Distribution</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Phosphorous Acids</term><term>Polyamines</term><term>Radioisotopes</term><term>Radiopharmaceuticals</term><term>Thulium</term></keywords><keywords scheme="MESH" qualifier="metabolism" xml:lang="en"><term>Bone and Bones</term></keywords><keywords scheme="MESH" qualifier="pathology" xml:lang="en"><term>Bone and Bones</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacokinetics" xml:lang="en"><term>Phosphorous Acids</term><term>Polyamines</term><term>Radioisotopes</term><term>Radiopharmaceuticals</term><term>Thulium</term></keywords><keywords scheme="MESH" qualifier="radionuclide imaging" xml:lang="en"><term>Bone and Bones</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Isotope Labeling</term><term>Palliative Care</term><term>Rats</term><term>Rats, Wistar</term><term>Tissue Distribution</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Thulium-170 [T1/2=128.4 days, Eβ(max)=968 keV, and Eγ=84 keV (3.26%)] could be considered an easily producible and cost-effective alternative to (89)Sr for the preparation of radiopharmaceuticals for palliation of bone pain arising due to skeletal metastases. Multidentate aminomethylene polyphosphonic acids have already been proven to be effective as carrier moieties for developing radiolabeled bone pain palliation agents using lanthanide radionuclides. Therefore, an attempt was made to evaluate the potential of a series of (170)Tm-labeled acyclic (diethylenetriaminepentamethylene phosphonic acid and triethylenetetraminehexamethylene phosphonic acid) and cyclic polyaminopolyphosphonic acids (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetramethylene phosphonic acid [DOTMP] and 1,4,8,11-tetraazacyclotetradecane-1,4,8,11-tetramethylene phosphonic acid [CTMP]) toward their use as alternative bone pain palliation agents.</div></front></TEI><pubmed><MedlineCitation Owner="NLM" Status="MEDLINE"><PMID Version="1">23931111</PMID><DateCreated><Year>2013</Year><Month>11</Month><Day>15</Day></DateCreated><DateCompleted><Year>2014</Year><Month>08</Month><Day>25</Day></DateCompleted><Article PubModel="Print-Electronic"><Journal><ISSN IssnType="Electronic">1557-8852</ISSN><JournalIssue CitedMedium="Internet"><Volume>28</Volume><Issue>10</Issue><PubDate><Year>2013</Year><Month>Dec</Month></PubDate></JournalIssue><Title>Cancer biotherapy & radiopharmaceuticals</Title><ISOAbbreviation>Cancer Biother. Radiopharm.</ISOAbbreviation></Journal><ArticleTitle>Radiolabeling, stability studies, and pharmacokinetic evaluation of thulium-170-labeled acyclic and cyclic polyaminopolyphosphonic acids.</ArticleTitle><Pagination><MedlinePgn>737-45</MedlinePgn></Pagination><ELocationID EIdType="doi" ValidYN="Y">10.1089/cbr.2013.1475</ELocationID><Abstract><AbstractText Label="OBJECTIVE" NlmCategory="OBJECTIVE">Thulium-170 [T1/2=128.4 days, Eβ(max)=968 keV, and Eγ=84 keV (3.26%)] could be considered an easily producible and cost-effective alternative to (89)Sr for the preparation of radiopharmaceuticals for palliation of bone pain arising due to skeletal metastases. Multidentate aminomethylene polyphosphonic acids have already been proven to be effective as carrier moieties for developing radiolabeled bone pain palliation agents using lanthanide radionuclides. Therefore, an attempt was made to evaluate the potential of a series of (170)Tm-labeled acyclic (diethylenetriaminepentamethylene phosphonic acid and triethylenetetraminehexamethylene phosphonic acid) and cyclic polyaminopolyphosphonic acids (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetramethylene phosphonic acid [DOTMP] and 1,4,8,11-tetraazacyclotetradecane-1,4,8,11-tetramethylene phosphonic acid [CTMP]) toward their use as alternative bone pain palliation agents.</AbstractText><AbstractText Label="EXPERIMENTAL" NlmCategory="METHODS">Thulium-170 was produced by irradiating the natural Tm2O3 target at a thermal neutron flux of 7×10(13) n·cm(-2)·s(-1) for a period of 60 days. All the phosphonic acid ligands were synthesized and characterized in-house. The protocols for radiolabeling the phosphonic acids with (170)Tm were standardized. Biological evaluation of the (170)Tm-labeled phosphonic acids were carried out in normal Wistar rats by biodistribution as well as by scintigraphic studies.</AbstractText><AbstractText Label="RESULTS" NlmCategory="RESULTS">Thulium-170 was produced with adequate specific activity (173 Ci/g, 6.41 TBq/g) and high radionuclidic purity (99.62%). All the (170)Tm-labeled phosphonic acids, except (170)Tm-CTMP, were prepared with very high radiochemical purity (>98%) under optimized reaction conditions and exhibited high stability. All the agents showed selective skeletal accumulation with insignificant uptake in other vital organs/tissues and major clearance through renal pathway. These findings were also substantiated by scintigraphic studies.</AbstractText><AbstractText Label="CONCLUSIONS" NlmCategory="CONCLUSIONS">Although all the (170)Tm-labeled phosphonic acids showed significant and selective skeletal accumulation, radiochemical studies indicate that (170)Tm-DOTMP is the best choice for carrying out further evaluation toward its use for clinical applications.</AbstractText></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Vats</LastName><ForeName>Kusum</ForeName><Initials>K</Initials><AffiliationInfo><Affiliation>1 Radiopharmaceuticals Division, Bhabha Atomic Research Centre , Mumbai, India .</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Das</LastName><ForeName>Tapas</ForeName><Initials>T</Initials></Author><Author ValidYN="Y"><LastName>Sarma</LastName><ForeName>Haladhar D</ForeName><Initials>HD</Initials></Author><Author ValidYN="Y"><LastName>Banerjee</LastName><ForeName>Sharmila</ForeName><Initials>S</Initials></Author><Author ValidYN="Y"><LastName>Pillai</LastName><ForeName>M R A</ForeName><Initials>MR</Initials></Author></AuthorList><Language>eng</Language><PublicationTypeList><PublicationType UI="D016428">Journal Article</PublicationType></PublicationTypeList><ArticleDate DateType="Electronic"><Year>2013</Year><Month>08</Month><Day>09</Day></ArticleDate></Article><MedlineJournalInfo><Country>United States</Country><MedlineTA>Cancer Biother Radiopharm</MedlineTA><NlmUniqueID>9605408</NlmUniqueID><ISSNLinking>1084-9785</ISSNLinking></MedlineJournalInfo><ChemicalList><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D010757">Phosphorous Acids</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D011073">Polyamines</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D011868">Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D019275">Radiopharmaceuticals</NameOfSubstance></Chemical><Chemical><RegistryNumber>13598-36-2</RegistryNumber><NameOfSubstance UI="C570063">phosphonic acid</NameOfSubstance></Chemical><Chemical><RegistryNumber>8RKC5ATI4P</RegistryNumber><NameOfSubstance UI="D013932">Thulium</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName MajorTopicYN="N" UI="D000818">Animals</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N" UI="D001842">Bone and Bones</DescriptorName><QualifierName MajorTopicYN="N" UI="Q000378">metabolism</QualifierName><QualifierName MajorTopicYN="N" UI="Q000473">pathology</QualifierName><QualifierName MajorTopicYN="Y" UI="Q000531">radionuclide imaging</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N" UI="D007553">Isotope Labeling</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N" UI="D010166">Palliative Care</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N" UI="D010757">Phosphorous Acids</DescriptorName><QualifierName MajorTopicYN="N" UI="Q000737">chemistry</QualifierName><QualifierName MajorTopicYN="Y" UI="Q000493">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N" UI="D011073">Polyamines</DescriptorName><QualifierName MajorTopicYN="N" UI="Q000737">chemistry</QualifierName><QualifierName MajorTopicYN="N" UI="Q000493">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N" UI="D011868">Radioisotopes</DescriptorName><QualifierName MajorTopicYN="N" UI="Q000737">chemistry</QualifierName><QualifierName MajorTopicYN="Y" UI="Q000493">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N" UI="D019275">Radiopharmaceuticals</DescriptorName><QualifierName MajorTopicYN="N" UI="Q000737">chemistry</QualifierName><QualifierName MajorTopicYN="Y" UI="Q000493">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N" UI="D051381">Rats</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N" UI="D017208">Rats, Wistar</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N" UI="D013932">Thulium</DescriptorName><QualifierName MajorTopicYN="Y" UI="Q000737">chemistry</QualifierName><QualifierName MajorTopicYN="Y" UI="Q000493">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N" UI="D014018">Tissue Distribution</DescriptorName></MeshHeading></MeshHeadingList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="aheadofprint"><Year>2013</Year><Month>8</Month><Day>9</Day></PubMedPubDate><PubMedPubDate 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