Desferrioxamine as an appropriate chelator for 90Nb: Comparison of its complexation properties for M-Df-Octreotide (M=Nb, Fe, Ga, Zr)

Radchenko, Valery; Busse, S.; Roesch, Frank

doi:10.1016/j.nucmedbio.2014.06.006

Cited by 19 publications

(14 citation statements)

References 18 publications

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“…The relatively short half-life of Ga-68 can be a limitation especially in longitudinal studies. This deficit can be resolved using longer-lived positron-emitting radionuclides such as Cu-64, I-124, Y-86, Nb-90 or Zr-89 [ 10 ].…”

Section: Introductionmentioning

confidence: 99%

In Vitro and In Vivo Comparison of Selected Ga-68 and Zr-89 Labelled Siderophores

et al. 2015

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PurposeSome [68Ga]siderophores show promise in specific and sensitive imaging of infection. Here, we compare the in vitro and in vivo behaviour of selected Ga-68 and Zr-89 labelled siderophores.ProceduresRadiolabelling was performed in HEPES or sodium acetate buffer systems. Radiochemical purity of labelled siderophores was determined using chromatography. Partition coefficients, in vitro stability and protein binding affinities were determined. Ex vivo biodistribution and animal imaging was studied in mice.ResultsCertain differences among studied siderophores were observed in labelling efficiency. Protein binding and stability tests showed highest stabilities and lowest protein binding affinities for Ga-68 and [89Zr]triacetylfusarinine C (TAFC). All studied Ga-68 and [89Zr]siderophores exhibited a similar biodistribution and pharmacokinetics in mice with the exception of [89Zr]ferrioxamine E (FOXE).ConclusionsZr-89 and [68Ga]siderophores showed analogous in vitro and in vivo behaviour. Tested [89Zr]siderophores could be applied for longitudinal positron emission tomography (PET) studies of fungal infections and especially TAFC for the development of novel bioconjugates.Electronic supplementary materialThe online version of this article (doi:10.1007/s11307-015-0897-6) contains supplementary material, which is available to authorized users.

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Section: Introductionmentioning

confidence: 99%

In Vitro and In Vivo Comparison of Selected Ga-68 and Zr-89 Labelled Siderophores

et al. 2015

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“…The coordination of 90 Nb with different chelators has been evaluated in terms of radiolabeling efficiency and stability of the radiolabeled Nb 5+ complex. 82 Results indicate that DFO shows the best properties as it is able to form quantitative complexes at a wide range of pHs (4-7) at room temperature. In addition, it was verified that bi-functionalization does not affect the complex formation parameters of the DFO and that the complex remains stable in vivo.…”

Section: Nb-90mentioning

confidence: 97%

“…In addition, it was verified that bi-functionalization does not affect the complex formation parameters of the DFO and that the complex remains stable in vivo. 82 In follow-up studies, the mAb rituximab was radiolabeled with 90 Nb, and stability measurements revealed that the complex was more than 99% stable over a prolonged period of 18 days. 83 Recently, as a proof of concept, 90 Nb was used to label the mAb bevacizumab (Avastin®), and in vitro and in vivo stability was evaluated in normal swiss mice and tumor-bearing SCID mice.…”

Section: Nb-90mentioning

confidence: 99%

PET radiometals for antibody labeling

Aluicio‐Sarduy

Ellison

Barnhart

et al. 2018

Labelled Comp Radiopharmac

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Recent advances in molecular characterization of tumors have made possible the emergence of new types of cancer therapies where traditional cytotoxic drugs and nonspecific chemotherapy can be complemented with targeted molecular therapies. One of the main revolutionary treatments is the use of monoclonal antibodies (mAbs) that selectively target the disseminated tumor cells while sparing normal tissues. mAbs and related therapeutics can be efficiently radiolabeled with a wide range of radionuclides to facilitate preclinical and clinical studies. Non-invasive molecular imaging techniques, such as Positron Emission Tomography (PET), using radiolabeled mAbs provide useful information on the whole-body distribution of the biomolecules, which may enable patient stratification, diagnosis, selection of targeted therapies, evaluation of treatment response, and prediction of dose limiting tissue and adverse effects. In addition, when mAbs are labeled with therapeutic radionuclides, the combination of immunological and radiobiological cytotoxicity may result in enhanced treatment efficacy. The pharmacokinetic profile of antibodies demands the use of long half-life isotopes for longitudinal scrutiny of mAb biodistribution and precludes the use of well-stablished short half-life isotopes. Herein, we review the most promising PET radiometals with chemical and physical characteristics that make the appealing for mAb labeling, highlighting those with theranostic radioisotopes.

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“…Desferrioxamine has been shown to be an appropriate chelate for Nb (Radchenko et al, 2014) Bevacizumab was pre-modified with the bifunctional chelator Df-Bz-NCS following the protocol for 89 Zr labelling from (Vosjan et al, 2010). In short, a threefold molar excess of Df-Bz-NCS (in 20 μL DMSO) was added to 5 mg of the mab in 1 ml 0.1 M NaHCO3 buffer, pH 9.0, and incubated for 30 min at 37 °C.…”

Section: Monoclonal Antibody Modification With Df-bz-ncsmentioning

confidence: 99%

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

Radchenko

Bouziotis

Tsotakos

et al. 2016

Nuclear Medicine and Biology

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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. (90)Nb is a promising candidate for in vivo immuno-PET, due its half-life of 14.6h and low β(+) energy of Emean=0.35MeV per decay. (95)Nb on the other hand, is a convenient alternative for longer-term ex vivo biodistribution studies, due to its longer half-life of (t½=35days) and its convenient, lower-cost production (reactor-based production). In this proof-of-principle work, the monoclonal antibody bevacizumab (Avastin(®)) was labeled with (95/90)Nb and in vitro and in vivo stability was evaluated in normal Swiss mice and in tumor-bearing SCID mice. Initial ex vivo experiments with (95)Nb-bevacizumab showed adequate tumor uptake, however at the same time high uptake in the liver, spleen and kidneys was observed. In order to investigate whether this behavior is due to instability of (⁎)Nb-bevacizumab or to the creation of other (⁎)Nb species in vivo, we performed biodistribution studies of (95)Nb-oxalate, (95)Nb-chloride and (95)Nb-Df. These potential metabolite species did not show any specific uptake, apart from bone accumulation for (95)Nb-oxalate and (95)Nb-chloride, which, interestingly, may serve as an "indicator" for the release of (90)Nb from labeled biomolecules. Concerning the initial uptake of (95)Nb-bevacizumab in non-tumor tissue, biodistribution of a higher specific activity radiolabeled antibody sample did show only negligible uptake in the liver, spleen, kidneys or bones. In-vivo imaging of a tumor-bearing SCID mouse after injection with (90)Nb-bevacizumab was acquired on an experimental small-animal PET camera, and indeed showed localization of the radiotracer in the tumor area. It is the first time that such results are described in the literature, and indicates promise of application of (90)Nb-labeled antibodies for the purposes of immuno-PET.

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Desferrioxamine as an appropriate chelator for 90Nb: Comparison of its complexation properties for M-Df-Octreotide (M=Nb, Fe, Ga, Zr)

Cited by 19 publications

References 18 publications

In Vitro and In Vivo Comparison of Selected Ga-68 and Zr-89 Labelled Siderophores

In Vitro and In Vivo Comparison of Selected Ga-68 and Zr-89 Labelled Siderophores

PET radiometals for antibody labeling

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

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