Preclinical development of a novel [68Ga]Ga-/[177Lu]Lu-labeled agent for PSMA-targeted imaging and therapy
Prostate-specific membrane antigen (PSMA)-targeted radiolabeled agents have been developed to diagnose and treat prostate cancer. In this study, we developed a novel 68 Ga-/ 177 Lu-labeled PSMA-targeted agent for potential for theranostics of prostate cancer. Methods:[ 68 Ga]Ga-/[ 177 Lu]Lu-PSMA-BP...
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| Veröffentlicht in: | Journal of radioanalytical and nuclear chemistry 2022-06, Vol.331 (6), p.2705-2717 |
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| creator | Wu, Yitian Zhang, Xiaojun Zhou, Haoxi Zhang, Jinming |
| description | Prostate-specific membrane antigen (PSMA)-targeted radiolabeled agents have been developed to diagnose and treat prostate cancer. In this study, we developed a novel
68
Ga-/
177
Lu-labeled PSMA-targeted agent for potential for theranostics of prostate cancer. Methods:[
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP were efficiently prepared manually. For in vitro cell experiments 22Rv1 (PSMA+) and PC-3 (PSMA-) cell lines were used. Biodistribution studies, small-animal SPECT imaging, Micro-PET imaging, and therapy studies of [
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP were conducted in mice bearing 22Rv1 and PC-3 xenografted tumors. Results:[
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP were prepared within 30 min. The binding affinity Ki value of PSMA-BP to PSMA was 8.34 ± 2.02 nM. Micro-PET and small-animal SPECT imaging showed accumulation of [
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP mainly in 22Rv1 tumors with a favorable clearance pattern from non-target oragans. Low radioactivity accumulation was observed in PC-3 tumors and PSMA-expressing tissues. The SUVmax for 22Rv1 tumor, PC-3 tumor were 0.77 ± 0.16, 0.09 ± 0.07. The uptake of
68
Ga-PSMA-BP in 22Rv1 tumors could be substantially blocked by 2-PMPA (− 81.82%). The mice treated with either low or high dose of
177
Lu-PSMA-BP showed delayed tumor growth. Conclusion: Our results demonstrated the promising theranostic potential of [
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP for prostate cancer, while the efficacy warranted further investigation to evaluate the potential for clinical application.
Graphical abstract |
| doi_str_mv | 10.1007/s10967-022-08301-5 |
| format | Article |
| fullrecord | <record><control><sourceid>gale_proqu</sourceid><recordid>TN_cdi_proquest_journals_2672359560</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><galeid>A705763496</galeid><sourcerecordid>A705763496</sourcerecordid><originalsourceid>FETCH-LOGICAL-c316t-a9667ba151610c7b09bba9fa22a716a0f5d5c665906ea3a8f366d4713e37a74a3</originalsourceid><addsrcrecordid>eNp9kdFqHCEUhqWk0E3aF-iV0GuTo646c7mEZFvY0kDbqxDkjKPTWWZ1o7OBffuabiEESvHiwM_3HcWfkI8cLjmAuSocWm0YCMGgkcCZekMWXDUNE6aBM7IAITVTRvJ35LyULQC0TSMXZHuXvZvGODqcaO-f_JT2Ox9nmgJFGlMN6L1u1viwRnZ1z43ZHB42BzZh5yffUxye4ZAyvfv-dcVmzIOfaz7ucBjjQDH2dP7lM-6P78nbgFPxH_7OC_Lz9ubH9We2-bb-cr3aMCe5nhm2WpsOueKagzMdtF2HbUAh0HCNEFSvnNaqBe1RYhOk1v3ScOmlQbNEeUE-nfbuc3o8-DLbbTrkWK-0QhshVas0vFADTt6OMaQ5o9uNxdmVAWW0XLa6Upf_oOrp_W50Kfow1vyVIE6Cy6mU7IPd5_oX-Wg52Oeq7KkqW6uyf6qyqkryJJUKx8Hnlxf_x_oN9OiTlA</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>2672359560</pqid></control><display><type>article</type><title>Preclinical development of a novel [68Ga]Ga-/[177Lu]Lu-labeled agent for PSMA-targeted imaging and therapy</title><source>SpringerLink Journals - AutoHoldings</source><creator>Wu, Yitian ; Zhang, Xiaojun ; Zhou, Haoxi ; Zhang, Jinming</creator><creatorcontrib>Wu, Yitian ; Zhang, Xiaojun ; Zhou, Haoxi ; Zhang, Jinming</creatorcontrib><description>Prostate-specific membrane antigen (PSMA)-targeted radiolabeled agents have been developed to diagnose and treat prostate cancer. In this study, we developed a novel
68
Ga-/
177
Lu-labeled PSMA-targeted agent for potential for theranostics of prostate cancer. Methods:[
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP were efficiently prepared manually. For in vitro cell experiments 22Rv1 (PSMA+) and PC-3 (PSMA-) cell lines were used. Biodistribution studies, small-animal SPECT imaging, Micro-PET imaging, and therapy studies of [
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP were conducted in mice bearing 22Rv1 and PC-3 xenografted tumors. Results:[
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP were prepared within 30 min. The binding affinity Ki value of PSMA-BP to PSMA was 8.34 ± 2.02 nM. Micro-PET and small-animal SPECT imaging showed accumulation of [
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP mainly in 22Rv1 tumors with a favorable clearance pattern from non-target oragans. Low radioactivity accumulation was observed in PC-3 tumors and PSMA-expressing tissues. The SUVmax for 22Rv1 tumor, PC-3 tumor were 0.77 ± 0.16, 0.09 ± 0.07. The uptake of
68
Ga-PSMA-BP in 22Rv1 tumors could be substantially blocked by 2-PMPA (− 81.82%). The mice treated with either low or high dose of
177
Lu-PSMA-BP showed delayed tumor growth. Conclusion: Our results demonstrated the promising theranostic potential of [
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP for prostate cancer, while the efficacy warranted further investigation to evaluate the potential for clinical application.
Graphical abstract</description><identifier>ISSN: 0236-5731</identifier><identifier>EISSN: 1588-2780</identifier><identifier>DOI: 10.1007/s10967-022-08301-5</identifier><language>eng</language><publisher>Cham: Springer International Publishing</publisher><subject>Accumulation ; Antigens ; Chemistry ; Chemistry and Materials Science ; Diagnostic Radiology ; Ethylenediaminetetraacetic acid ; Hadrons ; Heavy Ions ; Imaging ; Inorganic Chemistry ; Lutetium isotopes ; Mouse devices ; Nuclear Chemistry ; Nuclear Physics ; PET imaging ; Physical Chemistry ; Positron emission ; Prostate cancer ; SPECT imaging ; Tomography ; Tumors</subject><ispartof>Journal of radioanalytical and nuclear chemistry, 2022-06, Vol.331 (6), p.2705-2717</ispartof><rights>Akadémiai Kiadó, Budapest, Hungary 2022</rights><rights>COPYRIGHT 2022 Springer</rights><rights>Akadémiai Kiadó, Budapest, Hungary 2022.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c316t-a9667ba151610c7b09bba9fa22a716a0f5d5c665906ea3a8f366d4713e37a74a3</citedby><cites>FETCH-LOGICAL-c316t-a9667ba151610c7b09bba9fa22a716a0f5d5c665906ea3a8f366d4713e37a74a3</cites><orcidid>0000-0002-9425-5180</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s10967-022-08301-5$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s10967-022-08301-5$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>315,781,785,27929,27930,41493,42562,51324</link.rule.ids></links><search><creatorcontrib>Wu, Yitian</creatorcontrib><creatorcontrib>Zhang, Xiaojun</creatorcontrib><creatorcontrib>Zhou, Haoxi</creatorcontrib><creatorcontrib>Zhang, Jinming</creatorcontrib><title>Preclinical development of a novel [68Ga]Ga-/[177Lu]Lu-labeled agent for PSMA-targeted imaging and therapy</title><title>Journal of radioanalytical and nuclear chemistry</title><addtitle>J Radioanal Nucl Chem</addtitle><description>Prostate-specific membrane antigen (PSMA)-targeted radiolabeled agents have been developed to diagnose and treat prostate cancer. In this study, we developed a novel
68
Ga-/
177
Lu-labeled PSMA-targeted agent for potential for theranostics of prostate cancer. Methods:[
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP were efficiently prepared manually. For in vitro cell experiments 22Rv1 (PSMA+) and PC-3 (PSMA-) cell lines were used. Biodistribution studies, small-animal SPECT imaging, Micro-PET imaging, and therapy studies of [
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP were conducted in mice bearing 22Rv1 and PC-3 xenografted tumors. Results:[
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP were prepared within 30 min. The binding affinity Ki value of PSMA-BP to PSMA was 8.34 ± 2.02 nM. Micro-PET and small-animal SPECT imaging showed accumulation of [
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP mainly in 22Rv1 tumors with a favorable clearance pattern from non-target oragans. Low radioactivity accumulation was observed in PC-3 tumors and PSMA-expressing tissues. The SUVmax for 22Rv1 tumor, PC-3 tumor were 0.77 ± 0.16, 0.09 ± 0.07. The uptake of
68
Ga-PSMA-BP in 22Rv1 tumors could be substantially blocked by 2-PMPA (− 81.82%). The mice treated with either low or high dose of
177
Lu-PSMA-BP showed delayed tumor growth. Conclusion: Our results demonstrated the promising theranostic potential of [
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP for prostate cancer, while the efficacy warranted further investigation to evaluate the potential for clinical application.
Graphical abstract</description><subject>Accumulation</subject><subject>Antigens</subject><subject>Chemistry</subject><subject>Chemistry and Materials Science</subject><subject>Diagnostic Radiology</subject><subject>Ethylenediaminetetraacetic acid</subject><subject>Hadrons</subject><subject>Heavy Ions</subject><subject>Imaging</subject><subject>Inorganic Chemistry</subject><subject>Lutetium isotopes</subject><subject>Mouse devices</subject><subject>Nuclear Chemistry</subject><subject>Nuclear Physics</subject><subject>PET imaging</subject><subject>Physical Chemistry</subject><subject>Positron emission</subject><subject>Prostate cancer</subject><subject>SPECT imaging</subject><subject>Tomography</subject><subject>Tumors</subject><issn>0236-5731</issn><issn>1588-2780</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2022</creationdate><recordtype>article</recordtype><recordid>eNp9kdFqHCEUhqWk0E3aF-iV0GuTo646c7mEZFvY0kDbqxDkjKPTWWZ1o7OBffuabiEESvHiwM_3HcWfkI8cLjmAuSocWm0YCMGgkcCZekMWXDUNE6aBM7IAITVTRvJ35LyULQC0TSMXZHuXvZvGODqcaO-f_JT2Ox9nmgJFGlMN6L1u1viwRnZ1z43ZHB42BzZh5yffUxye4ZAyvfv-dcVmzIOfaz7ucBjjQDH2dP7lM-6P78nbgFPxH_7OC_Lz9ubH9We2-bb-cr3aMCe5nhm2WpsOueKagzMdtF2HbUAh0HCNEFSvnNaqBe1RYhOk1v3ScOmlQbNEeUE-nfbuc3o8-DLbbTrkWK-0QhshVas0vFADTt6OMaQ5o9uNxdmVAWW0XLa6Upf_oOrp_W50Kfow1vyVIE6Cy6mU7IPd5_oX-Wg52Oeq7KkqW6uyf6qyqkryJJUKx8Hnlxf_x_oN9OiTlA</recordid><startdate>20220601</startdate><enddate>20220601</enddate><creator>Wu, Yitian</creator><creator>Zhang, Xiaojun</creator><creator>Zhou, Haoxi</creator><creator>Zhang, Jinming</creator><general>Springer International Publishing</general><general>Springer</general><general>Springer Nature B.V</general><scope>AAYXX</scope><scope>CITATION</scope><orcidid>https://orcid.org/0000-0002-9425-5180</orcidid></search><sort><creationdate>20220601</creationdate><title>Preclinical development of a novel [68Ga]Ga-/[177Lu]Lu-labeled agent for PSMA-targeted imaging and therapy</title><author>Wu, Yitian ; Zhang, Xiaojun ; Zhou, Haoxi ; Zhang, Jinming</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c316t-a9667ba151610c7b09bba9fa22a716a0f5d5c665906ea3a8f366d4713e37a74a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2022</creationdate><topic>Accumulation</topic><topic>Antigens</topic><topic>Chemistry</topic><topic>Chemistry and Materials Science</topic><topic>Diagnostic Radiology</topic><topic>Ethylenediaminetetraacetic acid</topic><topic>Hadrons</topic><topic>Heavy Ions</topic><topic>Imaging</topic><topic>Inorganic Chemistry</topic><topic>Lutetium isotopes</topic><topic>Mouse devices</topic><topic>Nuclear Chemistry</topic><topic>Nuclear Physics</topic><topic>PET imaging</topic><topic>Physical Chemistry</topic><topic>Positron emission</topic><topic>Prostate cancer</topic><topic>SPECT imaging</topic><topic>Tomography</topic><topic>Tumors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Wu, Yitian</creatorcontrib><creatorcontrib>Zhang, Xiaojun</creatorcontrib><creatorcontrib>Zhou, Haoxi</creatorcontrib><creatorcontrib>Zhang, Jinming</creatorcontrib><collection>CrossRef</collection><jtitle>Journal of radioanalytical and nuclear chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Wu, Yitian</au><au>Zhang, Xiaojun</au><au>Zhou, Haoxi</au><au>Zhang, Jinming</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Preclinical development of a novel [68Ga]Ga-/[177Lu]Lu-labeled agent for PSMA-targeted imaging and therapy</atitle><jtitle>Journal of radioanalytical and nuclear chemistry</jtitle><stitle>J Radioanal Nucl Chem</stitle><date>2022-06-01</date><risdate>2022</risdate><volume>331</volume><issue>6</issue><spage>2705</spage><epage>2717</epage><pages>2705-2717</pages><issn>0236-5731</issn><eissn>1588-2780</eissn><abstract>Prostate-specific membrane antigen (PSMA)-targeted radiolabeled agents have been developed to diagnose and treat prostate cancer. In this study, we developed a novel
68
Ga-/
177
Lu-labeled PSMA-targeted agent for potential for theranostics of prostate cancer. Methods:[
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP were efficiently prepared manually. For in vitro cell experiments 22Rv1 (PSMA+) and PC-3 (PSMA-) cell lines were used. Biodistribution studies, small-animal SPECT imaging, Micro-PET imaging, and therapy studies of [
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP were conducted in mice bearing 22Rv1 and PC-3 xenografted tumors. Results:[
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP were prepared within 30 min. The binding affinity Ki value of PSMA-BP to PSMA was 8.34 ± 2.02 nM. Micro-PET and small-animal SPECT imaging showed accumulation of [
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP mainly in 22Rv1 tumors with a favorable clearance pattern from non-target oragans. Low radioactivity accumulation was observed in PC-3 tumors and PSMA-expressing tissues. The SUVmax for 22Rv1 tumor, PC-3 tumor were 0.77 ± 0.16, 0.09 ± 0.07. The uptake of
68
Ga-PSMA-BP in 22Rv1 tumors could be substantially blocked by 2-PMPA (− 81.82%). The mice treated with either low or high dose of
177
Lu-PSMA-BP showed delayed tumor growth. Conclusion: Our results demonstrated the promising theranostic potential of [
68
Ga]Ga-/[
177
Lu]Lu-PSMA-BP for prostate cancer, while the efficacy warranted further investigation to evaluate the potential for clinical application.
Graphical abstract</abstract><cop>Cham</cop><pub>Springer International Publishing</pub><doi>10.1007/s10967-022-08301-5</doi><tpages>13</tpages><orcidid>https://orcid.org/0000-0002-9425-5180</orcidid></addata></record> |
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| subjects | Accumulation Antigens Chemistry Chemistry and Materials Science Diagnostic Radiology Ethylenediaminetetraacetic acid Hadrons Heavy Ions Imaging Inorganic Chemistry Lutetium isotopes Mouse devices Nuclear Chemistry Nuclear Physics PET imaging Physical Chemistry Positron emission Prostate cancer SPECT imaging Tomography Tumors |
| title | Preclinical development of a novel [68Ga]Ga-/[177Lu]Lu-labeled agent for PSMA-targeted imaging and therapy |
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