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The radiolabeling of [161Tb]Tb-PSMA-617 by a novel radiolabeling method and preclinical evaluation by in vitro/in vivo methods
Prostate cancer (PC) is the most prevalent cancer in elderly men, exhibiting a positive correlation with age. As resistance to treatment has developed, particularly in the progressive stage of the disease and in the presence of microfocal multiple bone metastases, new generation radionuclide therapi...
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| Published in: | Journal of radioanalytical and nuclear chemistry 2024-10, Vol.333 (12), p.6403-6413 |
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| creator | Uygur, Emre Sezgin, Ceren Parlak, Yasemin Karatay, Kadriye Buşra Arıkbaşı, Bilal Avcıbaşı, Uğur Toklu, Türkay Barutça, Sabri Harmanşah, Coşkun Sözen, Tevfik Sinan Maus, Stephan Scher, Howard Aras, Omer Gümüşer, Fikriye Gül Biber Muftuler, Fazilet Zumrut |
| description | Prostate cancer (PC) is the most prevalent cancer in elderly men, exhibiting a positive correlation with age. As resistance to treatment has developed, particularly in the progressive stage of the disease and in the presence of microfocal multiple bone metastases, new generation radionuclide therapies have emerged. Recently introduced for treating micrometastatic foci, Terbium-161 ([
161
Tb]) has shown great promise in prostate cancer treatment. This study investigated the in vitro and in vivo cytotoxicity of Terbium-161 ([
161
Tb])-radiolabeled prostate-specific membrane antigen (PSMA)-617. [
161
Tb]Tb-PSMA-617 (7.4 MBq/nmol) demonstrated a radiochemical yield of 97.99 ± 2.01% and hydrophilicity. [
161
Tb]Tb-PSMA-617 was also shown to have good stability, with a radiochemical yield of over 95% up to 72 h. In vitro, [
161
Tb]Tb-PSMA-617 exhibited cytotoxicity on LNCaP cells but not on PC3 cells. In vivo, scintigraphy imaging visualized the accumulation of [
161
Tb]Tb-PSMA-617 in the prostate, kidneys, and bladder. The results suggest that [
161
Tb]Tb-PSMA-617 can be an effective radiolabeled agent for the treatment of PSMA positive foci in prostate cancer. |
| doi_str_mv | 10.1007/s10967-024-09809-8 |
| format | article |
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161
Tb]) has shown great promise in prostate cancer treatment. This study investigated the in vitro and in vivo cytotoxicity of Terbium-161 ([
161
Tb])-radiolabeled prostate-specific membrane antigen (PSMA)-617. [
161
Tb]Tb-PSMA-617 (7.4 MBq/nmol) demonstrated a radiochemical yield of 97.99 ± 2.01% and hydrophilicity. [
161
Tb]Tb-PSMA-617 was also shown to have good stability, with a radiochemical yield of over 95% up to 72 h. In vitro, [
161
Tb]Tb-PSMA-617 exhibited cytotoxicity on LNCaP cells but not on PC3 cells. In vivo, scintigraphy imaging visualized the accumulation of [
161
Tb]Tb-PSMA-617 in the prostate, kidneys, and bladder. The results suggest that [
161
Tb]Tb-PSMA-617 can be an effective radiolabeled agent for the treatment of PSMA positive foci in prostate cancer.</description><identifier>ISSN: 0236-5731</identifier><identifier>EISSN: 1588-2780</identifier><identifier>DOI: 10.1007/s10967-024-09809-8</identifier><language>eng</language><publisher>Cham: Springer International Publishing</publisher><subject>Biocompatibility ; Chemistry ; Chemistry and Materials Science ; Cytotoxicity ; Diagnostic Radiology ; Hadrons ; Heavy Ions ; In vitro methods and tests ; In vivo methods and tests ; Inorganic Chemistry ; Medical imaging ; Nuclear Chemistry ; Nuclear Physics ; Physical Chemistry ; Prostate cancer ; Radiochemistry ; Radioisotopes ; Radiolabelling ; Terbium ; Toxicity</subject><ispartof>Journal of radioanalytical and nuclear chemistry, 2024-10, Vol.333 (12), p.6403-6413</ispartof><rights>Akadémiai Kiadó, Budapest, Hungary 2024 Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law.</rights><rights>Copyright Springer Nature B.V. 2024</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><cites>FETCH-LOGICAL-c200t-759e82a4e7e0774f2aad2edae590021d69bfef141834ca9648f5c7c6bc8cf87f3</cites><orcidid>0000-0002-6791-9324 ; 0000-0003-1758-0542 ; 0000-0002-1941-0531 ; 0000-0003-2166-4490 ; 0000-0003-1679-8080 ; 0000-0002-3682-7611 ; 0000-0002-2573-3927 ; 0000-0002-8695-8759 ; 0000-0003-4946-8344 ; 0000-0001-8184-9660 ; 0000-0002-4777-9782 ; 0000-0002-3718-4195 ; 0000-0002-2811-4689 ; 0000-0001-7103-2323 ; 0000-0002-5399-9394</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids></links><search><creatorcontrib>Uygur, Emre</creatorcontrib><creatorcontrib>Sezgin, Ceren</creatorcontrib><creatorcontrib>Parlak, Yasemin</creatorcontrib><creatorcontrib>Karatay, Kadriye Buşra</creatorcontrib><creatorcontrib>Arıkbaşı, Bilal</creatorcontrib><creatorcontrib>Avcıbaşı, Uğur</creatorcontrib><creatorcontrib>Toklu, Türkay</creatorcontrib><creatorcontrib>Barutça, Sabri</creatorcontrib><creatorcontrib>Harmanşah, Coşkun</creatorcontrib><creatorcontrib>Sözen, Tevfik Sinan</creatorcontrib><creatorcontrib>Maus, Stephan</creatorcontrib><creatorcontrib>Scher, Howard</creatorcontrib><creatorcontrib>Aras, Omer</creatorcontrib><creatorcontrib>Gümüşer, Fikriye Gül</creatorcontrib><creatorcontrib>Biber Muftuler, Fazilet Zumrut</creatorcontrib><title>The radiolabeling of [161Tb]Tb-PSMA-617 by a novel radiolabeling method and preclinical evaluation by in vitro/in vivo methods</title><title>Journal of radioanalytical and nuclear chemistry</title><addtitle>J Radioanal Nucl Chem</addtitle><description>Prostate cancer (PC) is the most prevalent cancer in elderly men, exhibiting a positive correlation with age. As resistance to treatment has developed, particularly in the progressive stage of the disease and in the presence of microfocal multiple bone metastases, new generation radionuclide therapies have emerged. Recently introduced for treating micrometastatic foci, Terbium-161 ([
161
Tb]) has shown great promise in prostate cancer treatment. This study investigated the in vitro and in vivo cytotoxicity of Terbium-161 ([
161
Tb])-radiolabeled prostate-specific membrane antigen (PSMA)-617. [
161
Tb]Tb-PSMA-617 (7.4 MBq/nmol) demonstrated a radiochemical yield of 97.99 ± 2.01% and hydrophilicity. [
161
Tb]Tb-PSMA-617 was also shown to have good stability, with a radiochemical yield of over 95% up to 72 h. In vitro, [
161
Tb]Tb-PSMA-617 exhibited cytotoxicity on LNCaP cells but not on PC3 cells. In vivo, scintigraphy imaging visualized the accumulation of [
161
Tb]Tb-PSMA-617 in the prostate, kidneys, and bladder. The results suggest that [
161
Tb]Tb-PSMA-617 can be an effective radiolabeled agent for the treatment of PSMA positive foci in prostate cancer.</description><subject>Biocompatibility</subject><subject>Chemistry</subject><subject>Chemistry and Materials Science</subject><subject>Cytotoxicity</subject><subject>Diagnostic Radiology</subject><subject>Hadrons</subject><subject>Heavy Ions</subject><subject>In vitro methods and tests</subject><subject>In vivo methods and tests</subject><subject>Inorganic Chemistry</subject><subject>Medical imaging</subject><subject>Nuclear Chemistry</subject><subject>Nuclear Physics</subject><subject>Physical Chemistry</subject><subject>Prostate cancer</subject><subject>Radiochemistry</subject><subject>Radioisotopes</subject><subject>Radiolabelling</subject><subject>Terbium</subject><subject>Toxicity</subject><issn>0236-5731</issn><issn>1588-2780</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2024</creationdate><recordtype>article</recordtype><recordid>eNp9kE1LAzEQhoMoWKt_wFPAc-wk2d1kj6X4BRUF60kkZLNJu2W7qcl2oRd_u9sPEDx4mmF4nnfgReiawi0FEKNIIc8EAZYQyCXkRJ6gAU2lJExIOEUDYDwjqeD0HF3EuAToMckH6Hu2sDjosvK1LmxdNXPsHf6gGZ0Vn7OCvL49j0lGBS62WOPGd7b-g69su_Al1k2J18Ga_lYZXWPb6Xqj28o3O7VqcFe1wY_2S-ePVrxEZ07X0V4d5xC939_NJo9k-vLwNBlPiWEALRFpbiXTiRUWhEgc07pkttQ2zQEYLbO8cNbRhEqeGJ1niXSpESYrjDROCseH6OaQuw7-a2Njq5Z-E5r-peK9liacS9pT7ECZ4GMM1ql1qFY6bBUFtetZHXpWfc9q37OSvcQPUuzhZm7Db_Q_1g-xQoDg</recordid><startdate>20241028</startdate><enddate>20241028</enddate><creator>Uygur, Emre</creator><creator>Sezgin, Ceren</creator><creator>Parlak, Yasemin</creator><creator>Karatay, Kadriye Buşra</creator><creator>Arıkbaşı, Bilal</creator><creator>Avcıbaşı, Uğur</creator><creator>Toklu, Türkay</creator><creator>Barutça, Sabri</creator><creator>Harmanşah, Coşkun</creator><creator>Sözen, Tevfik Sinan</creator><creator>Maus, Stephan</creator><creator>Scher, Howard</creator><creator>Aras, Omer</creator><creator>Gümüşer, Fikriye Gül</creator><creator>Biber Muftuler, Fazilet Zumrut</creator><general>Springer International Publishing</general><general>Springer Nature B.V</general><scope>AAYXX</scope><scope>CITATION</scope><orcidid>https://orcid.org/0000-0002-6791-9324</orcidid><orcidid>https://orcid.org/0000-0003-1758-0542</orcidid><orcidid>https://orcid.org/0000-0002-1941-0531</orcidid><orcidid>https://orcid.org/0000-0003-2166-4490</orcidid><orcidid>https://orcid.org/0000-0003-1679-8080</orcidid><orcidid>https://orcid.org/0000-0002-3682-7611</orcidid><orcidid>https://orcid.org/0000-0002-2573-3927</orcidid><orcidid>https://orcid.org/0000-0002-8695-8759</orcidid><orcidid>https://orcid.org/0000-0003-4946-8344</orcidid><orcidid>https://orcid.org/0000-0001-8184-9660</orcidid><orcidid>https://orcid.org/0000-0002-4777-9782</orcidid><orcidid>https://orcid.org/0000-0002-3718-4195</orcidid><orcidid>https://orcid.org/0000-0002-2811-4689</orcidid><orcidid>https://orcid.org/0000-0001-7103-2323</orcidid><orcidid>https://orcid.org/0000-0002-5399-9394</orcidid></search><sort><creationdate>20241028</creationdate><title>The radiolabeling of [161Tb]Tb-PSMA-617 by a novel radiolabeling method and preclinical evaluation by in vitro/in vivo methods</title><author>Uygur, Emre ; 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As resistance to treatment has developed, particularly in the progressive stage of the disease and in the presence of microfocal multiple bone metastases, new generation radionuclide therapies have emerged. Recently introduced for treating micrometastatic foci, Terbium-161 ([
161
Tb]) has shown great promise in prostate cancer treatment. This study investigated the in vitro and in vivo cytotoxicity of Terbium-161 ([
161
Tb])-radiolabeled prostate-specific membrane antigen (PSMA)-617. [
161
Tb]Tb-PSMA-617 (7.4 MBq/nmol) demonstrated a radiochemical yield of 97.99 ± 2.01% and hydrophilicity. [
161
Tb]Tb-PSMA-617 was also shown to have good stability, with a radiochemical yield of over 95% up to 72 h. In vitro, [
161
Tb]Tb-PSMA-617 exhibited cytotoxicity on LNCaP cells but not on PC3 cells. In vivo, scintigraphy imaging visualized the accumulation of [
161
Tb]Tb-PSMA-617 in the prostate, kidneys, and bladder. The results suggest that [
161
Tb]Tb-PSMA-617 can be an effective radiolabeled agent for the treatment of PSMA positive foci in prostate cancer.</abstract><cop>Cham</cop><pub>Springer International Publishing</pub><doi>10.1007/s10967-024-09809-8</doi><tpages>11</tpages><orcidid>https://orcid.org/0000-0002-6791-9324</orcidid><orcidid>https://orcid.org/0000-0003-1758-0542</orcidid><orcidid>https://orcid.org/0000-0002-1941-0531</orcidid><orcidid>https://orcid.org/0000-0003-2166-4490</orcidid><orcidid>https://orcid.org/0000-0003-1679-8080</orcidid><orcidid>https://orcid.org/0000-0002-3682-7611</orcidid><orcidid>https://orcid.org/0000-0002-2573-3927</orcidid><orcidid>https://orcid.org/0000-0002-8695-8759</orcidid><orcidid>https://orcid.org/0000-0003-4946-8344</orcidid><orcidid>https://orcid.org/0000-0001-8184-9660</orcidid><orcidid>https://orcid.org/0000-0002-4777-9782</orcidid><orcidid>https://orcid.org/0000-0002-3718-4195</orcidid><orcidid>https://orcid.org/0000-0002-2811-4689</orcidid><orcidid>https://orcid.org/0000-0001-7103-2323</orcidid><orcidid>https://orcid.org/0000-0002-5399-9394</orcidid></addata></record> |
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| source | Springer Nature |
| subjects | Biocompatibility Chemistry Chemistry and Materials Science Cytotoxicity Diagnostic Radiology Hadrons Heavy Ions In vitro methods and tests In vivo methods and tests Inorganic Chemistry Medical imaging Nuclear Chemistry Nuclear Physics Physical Chemistry Prostate cancer Radiochemistry Radioisotopes Radiolabelling Terbium Toxicity |
| title | The radiolabeling of [161Tb]Tb-PSMA-617 by a novel radiolabeling method and preclinical evaluation by in vitro/in vivo methods |
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