Pretargeted radiopharmaceutical therapy Book Section
| Authors: | Keinänen, O. M.; Zeglis, B. M. |
| Editors: | Bodei, L.; Lewis, J. S.; Zeglis, B. M. |
| Article/Chapter Title: | Pretargeted radiopharmaceutical therapy |
| Abstract: | Radioimmunotherapy (RIT) has long stood as a promising approach to radiopharmaceutical therapy (RPT). However, the relatively slow pharmacokinetic profile of full-length radioimmunoconjugates can lead to toxic radiation doses to off-target organs. In pretargeted radioimmunotherapy (PRIT), the antibody and the radionuclide are decoupled, the former is administered hours to days ahead of the latter, and the two components undergo a selective ligation at the tumor site. Several approaches to PRIT have been developed over the past three decades, each based on a pair of moieties-a “molecular couple”-that react with one another in vivo with high specificity and affinity. All PRIT strategies follow the same general steps. First, the antibody bearing one half of the molecular couple is administered. Then, after the antibody has cleared from the blood and non-target organs, a radiolabeled variant of the complementary half of the molecular couple is injected. This radioligand, by design a small molecule, travels through the body quickly and either undergoes a ligation with the immunoconjugate at the tumor or is rapidly excreted. This approach is designed to deliver high radiation doses to tumor tissue while simultaneously minimizing the irradiation of healthy organs. In this chapter, we will provide examples of the use of in vivo pretargeting in nuclear medicine and discuss the most common approaches to in vivo pretargeting, including strategies based on streptavidin and biotin, bispecific antibodies, complementary oligonucleotides, and biorthogonal click chemistry. © The Editor(s) (if applicable) and The Author(s), under exclusive license to Springer Nature Switzerland AG 2023. |
| Keywords: | streptavidin; biotin; pretargeted radioimmunotherapy; bispecific antibody; pretargeting; multistep targeting; bioorthogonal click chemistry; inverse electron-demand diels-alder reaction; pretargeted radiopharmaceutical therapy |
| Book Title: | Radiopharmaceutical Therapy |
| ISBN: | 978-3-031-39004-3 |
| Publisher: | Springer |
| Publication Place: | Cham, Switzerland |
| Date Published: | 2023-01-01 |
| Start Page: | 435 |
| End Page: | 454 |
| Language: | English |
| DOI: | 10.1007/978-3-031-39005-0_21 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | Book chapter: 21 -- Source: Scopus |
Altmetric
Citation Impact
BMJ Impact Analytics
Related MSK Work