Lead-212 Radiopharmaceuticals for Receptor-Targeted Radionuclide Therapy
Receptor-targeted radionuclide therapy (RTRT) combines the power of particle-emitting radionuclides with the receptor-targeting capabilities of biomolecules, including antibodies and peptides. There are numerous radionuclides, but only a handful possess the necessary characteristics for targeted alp...
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Mazandaran University of Medical Sciences
2025-01-01
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| Series: | Journal of Mazandaran University of Medical Sciences |
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| Online Access: | http://jmums.mazums.ac.ir/article-1-21231-en.pdf |
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| author | Solmaz Mojarad-Jabali Sajjad Molavipordanjani |
| author_facet | Solmaz Mojarad-Jabali Sajjad Molavipordanjani |
| author_sort | Solmaz Mojarad-Jabali |
| collection | DOAJ |
| description | Receptor-targeted radionuclide therapy (RTRT) combines the power of particle-emitting radionuclides with the receptor-targeting capabilities of biomolecules, including antibodies and peptides. There are numerous radionuclides, but only a handful possess the necessary characteristics for targeted alpha therapy (TAT). Among them are actinium-225 (²²⁵Ac), bismuth-213 (²¹³Bi), radium-224 (²²⁴Ra), lead-212 (²¹²Pb), thorium-227 (²²⁷Th), astatine-211 (²¹¹At), and terbium-149 (¹⁴⁹Tb). Lead-212 (²¹²Pb) is a radionuclide that release both alpha and beta particles during its decay. The distinctive properties of ²¹²Pb, such as its relatively short half-life (10.64 hours), the commercial availability of ²²⁴Ra/²¹²Pb generators, in vivo generation of alpha particles through ²¹²Bi at its target site, simple conjugating process, and strong binding to chelators such as DOTA and TCMC make this radionuclide particularly promising for targeted alpha therapy. TAT with ²¹²Pb has demonstrated significant therapeutic effectiveness in both in vitro and in vivo models. To date, numerous biological molecules, including antibodies and peptides, have been labeled with ²¹²Pb in preclinical studies to evaluate their therapeutic efficacy and receptor-targeting potential. These studies have focused on receptors such as the epidermal growth factor receptor (EGFR) family, somatostatin receptor 2 (SSTR2), melanocortin 1 receptor (MC1R), prostate-specific membrane antigen (PSMA), CD37, CD38, CD46, vascular cell adhesion molecule 1 (VCAM-1), and chondroitin sulfate proteoglycan 4 (CSPG4). This review will first examine the physical properties of ²¹²Pb, followed by an analysis of its chemical characteristics, particularly its interactions with DOTA and TCMC. Finally, it will explore preclinical studies on ²¹²Pb-radiolabeled molecules and assess the clinical applications of radiotracers developed for receptor-targeted radionuclide therapy. |
| format | Article |
| id | doaj-art-66ea2b28da414ce7a754b969047198a2 |
| institution | DOAJ |
| issn | 1735-9260 1735-9279 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | Mazandaran University of Medical Sciences |
| record_format | Article |
| series | Journal of Mazandaran University of Medical Sciences |
| spelling | doaj-art-66ea2b28da414ce7a754b969047198a22025-08-20T03:11:48ZengMazandaran University of Medical SciencesJournal of Mazandaran University of Medical Sciences1735-92601735-92792025-01-0134241133148Lead-212 Radiopharmaceuticals for Receptor-Targeted Radionuclide TherapySolmaz Mojarad-Jabali0Sajjad Molavipordanjani1 Assistant Professor, Pharmaceutical Sciences Research Center, Mazandaran University of Medical Sciences, Sari, Iran Assistant Professor, Pharmaceutical Sciences Research Center, Mazandaran University of Medical Sciences, Sari, Iran Receptor-targeted radionuclide therapy (RTRT) combines the power of particle-emitting radionuclides with the receptor-targeting capabilities of biomolecules, including antibodies and peptides. There are numerous radionuclides, but only a handful possess the necessary characteristics for targeted alpha therapy (TAT). Among them are actinium-225 (²²⁵Ac), bismuth-213 (²¹³Bi), radium-224 (²²⁴Ra), lead-212 (²¹²Pb), thorium-227 (²²⁷Th), astatine-211 (²¹¹At), and terbium-149 (¹⁴⁹Tb). Lead-212 (²¹²Pb) is a radionuclide that release both alpha and beta particles during its decay. The distinctive properties of ²¹²Pb, such as its relatively short half-life (10.64 hours), the commercial availability of ²²⁴Ra/²¹²Pb generators, in vivo generation of alpha particles through ²¹²Bi at its target site, simple conjugating process, and strong binding to chelators such as DOTA and TCMC make this radionuclide particularly promising for targeted alpha therapy. TAT with ²¹²Pb has demonstrated significant therapeutic effectiveness in both in vitro and in vivo models. To date, numerous biological molecules, including antibodies and peptides, have been labeled with ²¹²Pb in preclinical studies to evaluate their therapeutic efficacy and receptor-targeting potential. These studies have focused on receptors such as the epidermal growth factor receptor (EGFR) family, somatostatin receptor 2 (SSTR2), melanocortin 1 receptor (MC1R), prostate-specific membrane antigen (PSMA), CD37, CD38, CD46, vascular cell adhesion molecule 1 (VCAM-1), and chondroitin sulfate proteoglycan 4 (CSPG4). This review will first examine the physical properties of ²¹²Pb, followed by an analysis of its chemical characteristics, particularly its interactions with DOTA and TCMC. Finally, it will explore preclinical studies on ²¹²Pb-radiolabeled molecules and assess the clinical applications of radiotracers developed for receptor-targeted radionuclide therapy.http://jmums.mazums.ac.ir/article-1-21231-en.pdfrtrttatradionuclide212pbradiotracersradionuclide therapy |
| spellingShingle | Solmaz Mojarad-Jabali Sajjad Molavipordanjani Lead-212 Radiopharmaceuticals for Receptor-Targeted Radionuclide Therapy Journal of Mazandaran University of Medical Sciences rtrt tat radionuclide 212pb radiotracers radionuclide therapy |
| title | Lead-212 Radiopharmaceuticals for Receptor-Targeted Radionuclide Therapy |
| title_full | Lead-212 Radiopharmaceuticals for Receptor-Targeted Radionuclide Therapy |
| title_fullStr | Lead-212 Radiopharmaceuticals for Receptor-Targeted Radionuclide Therapy |
| title_full_unstemmed | Lead-212 Radiopharmaceuticals for Receptor-Targeted Radionuclide Therapy |
| title_short | Lead-212 Radiopharmaceuticals for Receptor-Targeted Radionuclide Therapy |
| title_sort | lead 212 radiopharmaceuticals for receptor targeted radionuclide therapy |
| topic | rtrt tat radionuclide 212pb radiotracers radionuclide therapy |
| url | http://jmums.mazums.ac.ir/article-1-21231-en.pdf |
| work_keys_str_mv | AT solmazmojaradjabali lead212radiopharmaceuticalsforreceptortargetedradionuclidetherapy AT sajjadmolavipordanjani lead212radiopharmaceuticalsforreceptortargetedradionuclidetherapy |