targeted radionuclide therapy
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2022 ◽  
Author(s):  
Diana Melis ◽  
Andrew Burgoyne ◽  
Maarten Ooms ◽  
Gilles Gasser

Targeted radionuclide therapy (TRNT) is an ever-expanding field of nuclear medicine that provides a personalised approach to cancer treatment while limiting toxicity to normal tissues. It involves the radiolabelling of...


2022 ◽  
pp. 977-986
Author(s):  
Ø.S. Bruland ◽  
M.E. Revheim ◽  
R.H. Larsen ◽  
A. Juzeniene

2021 ◽  
Vol 66 (6) ◽  
pp. 63-70
Author(s):  
M. Vorontsova ◽  
T. Karmakova ◽  
A. Pankratov ◽  
A. Kaprin

Introduction 1. Features of Targeted Delivery of Therapeutic Radionuclides 2. Design of Pharmaceuticals for Targeted Radionuclide Therapy (TRT) 2.1. Radionuclides 2.2. Synthesis of Radioconjugates 2.3. Targeting Carriers 4. Subcellular Targeting of Radionuclides 5. TRT Dosimetry Conclusion


Molecules ◽  
2021 ◽  
Vol 26 (24) ◽  
pp. 7513
Author(s):  
Isidro Da Silva ◽  
Taylor R. Johnson ◽  
Jason C. Mixdorf ◽  
Eduardo Aluicio-Sarduy ◽  
Todd E. Barnhart ◽  
...  

Background: Radionuclides emitting Auger electrons (AEs) with low (0.02–50 keV) energy, short (0.0007–40 µm) range, and high (1–10 keV/µm) linear energy transfer may have an important role in the targeted radionuclide therapy of metastatic and disseminated disease. Erbium-165 is a pure AE-emitting radionuclide that is chemically matched to clinical therapeutic radionuclide 177Lu, making it a useful tool for fundamental studies on the biological effects of AEs. This work develops new biomedical cyclotron irradiation and radiochemical isolation methods to produce 165Er suitable for targeted radionuclide therapeutic studies and characterizes a new such agent targeting prostate-specific membrane antigen. Methods: Biomedical cyclotrons proton-irradiated spot-welded Ho(m) targets to produce 165Er, which was isolated via cation exchange chromatography (AG 50W-X8, 200–400 mesh, 20 mL) using alpha-hydroxyisobutyrate (70 mM, pH 4.7) followed by LN2 (20–50 µm, 1.3 mL) and bDGA (50–100 µm, 0.2 mL) extraction chromatography. The purified 165Er was radiolabeled with standard radiometal chelators and used to produce and characterize a new AE-emitting radiopharmaceutical, [165Er]PSMA-617. Results: Irradiation of 80–180 mg natHo targets with 40 µA of 11–12.5 MeV protons produced 165Er at 20–30 MBq·µA−1·h−1. The 4.9 ± 0.7 h radiochemical isolation yielded 165Er in 0.01 M HCl (400 µL) with decay-corrected (DC) yield of 64 ± 2% and a Ho/165Er separation factor of (2.8 ± 1.1) · 105. Radiolabeling experiments synthesized [165Er]PSMA-617 at DC molar activities of 37–130 GBq·µmol−1. Conclusions: A 2 h biomedical cyclotron irradiation and 5 h radiochemical separation produced GBq-scale 165Er suitable for producing radiopharmaceuticals at molar activities satisfactory for investigations of targeted radionuclide therapeutics. This will enable fundamental radiation biology experiments of pure AE-emitting therapeutic radiopharmaceuticals such as [165Er]PSMA-617, which will be used to understand the impact of AEs in PSMA-targeted radionuclide therapy of prostate cancer.


2021 ◽  
Vol 92 ◽  
pp. 52-61
Author(s):  
Giuseppe Della Gala ◽  
Manuel Bardiès ◽  
Jill Tipping ◽  
Lidia Strigari

Cancers ◽  
2021 ◽  
Vol 13 (22) ◽  
pp. 5776
Author(s):  
Elisabeth von Guggenberg ◽  
Petra Kolenc ◽  
Christof Rottenburger ◽  
Renata Mikołajczak ◽  
Alicja Hubalewska-Dydejczyk

The cholecystokinin-2 receptor (CCK2R) has been a target of interest for molecular imaging and targeted radionuclide therapy for two decades. However, so far CCK2R targeted imaging and therapy has not been introduced in clinical practice. Within this review the recent radiopharmaceutical development of CCK2R targeting compounds and the ongoing clinical trials are presented. Currently, new gastrin derivatives as well as nonpeptidic substances are being developed to improve the properties for clinical use. A team of specialists from the field of radiopharmacy and nuclear medicine reviewed the available literature and summarized their own experiences in the development and clinical testing of CCK2R targeting radiopharmaceuticals. The recent clinical trials with novel radiolabeled minigastrin analogs demonstrate the potential for both applications, imaging as well as targeted radiotherapy, and reinforce the clinical applicability within a theranostic concept. The intense efforts in optimizing CCK2R targeting radiopharmaceuticals has led to new substances for clinical use, as shown in first imaging studies in patients with advanced medullary thyroid cancer. The first clinical results suggest that the wider clinical implication of CCK2R-targeted radiopharmaceuticals is reasonable.


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