Preclinical Evaluation of Gastrin-Releasing Peptide Receptor Antagonists Labeled with Tb and Lu: A Comparative Study.

To elucidate potential benefits of the Auger-electron-emitting radionuclide Tb, we compared the preclinical performance of the gastrin-releasing peptide receptor antagonists RM2 (DOTA-Pip-d-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH) and AMTG (α-Me-Trp-RM2), each labeled with both Lu and Tb. Tb/Lu labeling (90°C, 5 min) and cell-based experiments (PC-3 cells) were performed. In vivo stability (30 min after injection) and biodistribution studies (1-72 h after injection) were performed on PC-3 tumor-bearing CB17-SCID mice.

Core-shell structured gold nanoparticles as carrier for Dy/Ho in vivo generator.

Background: Radionuclide therapy (RNT) has become a very important treatment modality for cancer nowadays. Comparing with other cancer treatment options, sufficient efficacy could be achieved in RNT with lower toxicity. β emitters are frequently used in RNT due to the long tissue penetration depth of the β particles.

Production of Sm-153 With Very High Specific Activity for Targeted Radionuclide Therapy.

Samarium-153 (Sm) is a highly interesting radionuclide within the field of targeted radionuclide therapy because of its favorable decay characteristics. Sm has a half-life of 1.93 d and decays into a stable daughter nuclide (Eu) whereupon β particles [E = 705 keV (30%), 635 keV (50%)] are emitted which are suitable for therapy.

Large-scale production of lutetium-177m for the Lu/Lu radionuclide generator.

In this work, Lu has been produced by irradiation of natural LuO targets at the BR2 reactor (Mol, Belgium) and the obtained data together with literature values have been used to theoretically investigate the production of Lu at different neutron fluxes, irradiation times and enrichment of Lu. The irradiation time (t) needed to reach the maximum Lu production has been found to change from 42, 12, 4 days with the increase in the thermal neutron flux from 2*10, 8*10, 2.5*10 n cm s, respectively while keeping the maximum Lu activity unaffected.

Therapeutic Potential of Sc in Comparison to Lu and Y: Preclinical Investigations.

Targeted radionuclide therapy with Lu- and Y-labeled radioconjugates is a clinically-established treatment modality for metastasized cancer. Sc is a therapeutic radionuclide that decays with a half-life of 3.35 days and emits medium-energy β-particles.

Sc for labeling of DOTA- and NODAGA-functionalized peptides: preclinical in vitro and in vivo investigations.

Background: Recently, Sc (T = 3.97 h, Eβ = 632 keV, I = 94.3 %) has emerged as an attractive radiometal candidate for PET imaging using DOTA-functionalized biomolecules.

Sc as useful β-emitter for the radiotheragnostic paradigm: a comparative study of feasible production routes.

Background: Radiotheragnostics makes use of the same molecular targeting vectors, labeled either with a diagnostic or therapeutic radionuclide, ideally of the same chemical element. The matched pair of scandium radionuclides, Sc and Sc, satisfies the desired physical aspects for PET imaging and radionuclide therapy, respectively. While the production and application of Sc was extensively studied, Sc is still in its infancy.

Labeling and preliminary in vivo assessment of niobium-labeled radioactive species: A proof-of-concept study.

The application of radionuclide-labeled biomolecules such as monoclonal antibodies or antibody fragments for imaging purposes is called immunoscintigraphy. More specifically, when the nuclides used are positron emitters, such as zirconium-89, the technique is referred to as immuno-PET. Currently, there is an urgent need for radionuclides with a half-life which correlates well with the biological kinetics of the biomolecules under question and which can be attached to the proteins by robust labeling chemistry.

The necessity of nuclear reactors for targeted radionuclide therapies.

Nuclear medicine has been contributing towards personalized therapies. Nuclear reactors are required for the working horses of both diagnosis and treatment, i.e.

Development of 177Lu-nanobodies for radioimmunotherapy of HER2-positive breast cancer: evaluation of different bifunctional chelators.

Nanobodies show favourable pharmacokinetic characteristics for tumor targeting, including high tumor-to-background-ratios. Labelled with a therapeutic radionuclide, nanobodies could be used as an adjuvant treatment option for HER2-overexpressing minimal residual disease. The therapeutic radionuclide Lutetium-177 is linked to the nanobody using a bifunctional chelator.