In Vivo Evaluation of a Bombesin Analogue Labeled with Ga-68 and Co-55/57

Dam, Johan Hygum; Olsen, Birgitte Brinkmann; Baun, Christina; Høilund‐Carlsen, Poul Flemming; Thisgaard, Helge

doi:10.1007/s11307-015-0911-z

Cited by 21 publications

(39 citation statements)

References 29 publications

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“…The presented method separates 55 Co in 400 μL, a volume that can be quickly evaporated even in the original 1.5 mL vial where the separated fractions are collected, which avoids the use of a large vessel (> 10 mL) connected to a roto-evaporator in which a variable loss of radioactivity may be lost in the large surface area of the glassware as it is difficult to re-dissolve all the activity off the walls of the vessel with a small volume (< 1 mL) of diluted HCl acid. Similarly, in the presented separation method of radio-cobalt from bulk iron, the use of the DGA branched extraction resin in the second part of the separation allows for: 1) the almost complete removal of radio-manganese impurities; and 2) a separated radio-cobalt that is concentrated in a small volume (0.4–0.6 mL) and has an effective specific activity with NOTA that is comparable to the highest one that has been reported using a NOTA-conjugated peptide (Dam et al, 2016). However, regarding the radionuclidic purity of 55 Co, the 58 Ni(p,α) route is worse than the 54 Fe(d,n) one due to the unavoidable presence of MBq amounts of 57 Co from 58 Ni(p,pn) 57 Ni→ 57 Co and from the 60 Ni(p,α) reaction on the 0.505% impurity of 60 Ni in the target material.…”

Section: Resultsmentioning

confidence: 99%

“…Cobalt-55 ( t 1/2 = 17.53 h, 76% β + , E max = 1498 keV) is an intermediate-lived positron-emitting radionuclide that is a useful radiotracer for positron emission tomography (PET) (De Reuck et al, 2004, 1999; Jansen et al, 1997a, 1997b, 1994, 1996b, 1995; Korf et al, 1998; Stevens et al, 1999) and particularly useful for labeling proteins due to its favorable complexation with established bifunctional chelators (Dam et al, 2016; Garousi et al, 2017; Mastren et al, 2015; Srivastava et al, 1994; Thisgaard et al, 2011b; Wallberg et al, 2010). Furthermore, when chelated in oxidation state 3+, the formed complex is considered inert (Duckworth et al, 2009; Regoeczi et al, 1995; Wegner and Spatz, 2013) and therefore it is less prone to interact with ligands in blood plasma and non-targeted organs due to trans-chelation.…”

Section: Introductionmentioning

confidence: 99%

“…So far, only seven studies have followed this chelator-based approach (Dam et al, 2016; Garousi et al, 2017; Goethals et al, 2000; Mastren et al, 2015; Srivastava et al, 1994; Thisgaard et al, 2011b; Wallberg et al, 2010). Goethals et al (Goethals et al, 2000) labeled 55 Co to ethylene diamine tetraacetic acid (EDTA) and characterized this complex for the application in the measurement of the glomerular filtration rate in kidneys via PET, a study which is commonly performed with the perfusion tracer 51 Cr-EDTA (Chantler et al, 1969).…”

Section: Introductionmentioning

confidence: 99%

“…Srivastava et al (1994), Thisgaard et al (2011b) and Mastren et al (2015) successfully labeled 55 Co to bifunctional chelators (BFC) conjugated to targeting peptides or proteins, although with very low effective specific activities (ESA): 3.7, 0.21, and 2.0 GBq/μmol, respectively. Dam et al (2016), has reported the highest ESA of 55 Co at 30 GBq/μmol by labeling a NOTA-conjugated bombesin analog under microwave heating in order to accelerate the labeling reaction.…”

Section: Introductionmentioning

confidence: 99%

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Cyclotron production and radiochemical separation of 55Co and 58mCo from 54Fe, 58Ni and 57Fe targets

Valdovinos

Hernandez

Graves

et al. 2017

Applied Radiation and Isotopes

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This work presents the production with a cyclotron of the positron emitter 55Co via the 54Fe(d,n) and 58Ni(p,α) reactions and the Auger electron emitter 58mCo via the 57Fe(d,n) reaction after high current (40 μA p and 60 μA d) irradiation on electroplated targets. High specific activity radionuclides (up to 55.6 GBq/μmol 55Co and 31.8 GBq/μmol 58mCo) with high radionuclidic purity (99.995% 55Co from 54Fe, 98.8% 55Co from 58Ni, and 98.7% 58mCo from 57Fe at end of bombardment, EoB), in high activity concentration (final separated radionuclide in < 0.6 mL) and with almost quantitative overall activity separation yield (> 92%) were obtained after processing of the irradiated targets with novel radiochemical separation methods based on HCl dissolution and the resin N,N,N′,N′-tetrakis-2-ethylhexyldiglycolamide (DGA, branched). One hour long irradiations using 38–65, 110–214 and 59–78 mg of enriched 54Fe (99.93%), 58Ni (99.48%) and 57Fe (95.06%), respectively, electroplated over a 1.0 cm2 surface, yielded 582 ± 66 MBq 55Co, 372 ± 14 MBq 55Co and 810 ± 186 MBq 58mCo, respectively, decay corrected to EoB. The separation methods allow for the recovery of the costly enriched target materials, which were reconstituted into metallic targets after novel electroplating methods, with an overall recycling efficiency of 93 ± 4% for iron. The produced radionuclides were used to radiolabel the angiogenesis marker antibody TRC105 conjugated to the chelator NOTA as a demonstration of their quality.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Cyclotron production and radiochemical separation of 55Co and 58mCo from 54Fe, 58Ni and 57Fe targets

Valdovinos

Hernandez

Graves

et al. 2017

Applied Radiation and Isotopes

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“…The potential use of GRPR-binding peptides in the prediction of surgical margin and metastatic lymph nodes was not addressed so far. The conventional imaging techniques used in preclinical studies never revealed a metastatic lymph node and precise surgical margin in live animals161718. But radiolabelled peptides were able to detect metastatic lymph nodes in patients1519.…”

mentioning

confidence: 99%

TM1-IR680 peptide for assessment of surgical margin and lymph node metastasis in murine orthotopic model of oral cancer

Kochurani

Nair

et al. 2016

Sci Rep

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Treatment outcome after surgical removal in oral carcinoma is poor due to inadequate methodologies available for marking surgical margins. Even though some methodologies for intraoperative margin assessment are under clinical and preclinical trials for other solid tumours, a promising modality for oral cancer surgery is not developed. Fluorescent-based optical imaging using Near Infrared (NIR) dyes tagged to tumour specific target will be an optimal tool for this purpose. One such target, Gastrin Releasing Peptide Receptor (GRPR) was selected for the study, and its binding peptide, TM1-IR680, was tested for its efficacy for surgical margin prediction in murine orthotopic model of oral cancer, derived from primary samples. Here, for the first time in a preclinical analysis, we show that the size and margin of oral cancer can be predicted, as revealed by 3D-imaging. Interestingly, the peptide was sensitive enough to detect lymph nodes that harboured dispersed tumour cells before colonization, which was impossible to identify by conventional histopathology. We recommend the use of TM1-NIR dyes alone or in combination with other technologies to improve the clinical outcome of oral cancer surgery.

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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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In Vivo Evaluation of a Bombesin Analogue Labeled with Ga-68 and Co-55/57

Cited by 21 publications

References 29 publications

Cyclotron production and radiochemical separation of 55Co and 58mCo from 54Fe, 58Ni and 57Fe targets

Cyclotron production and radiochemical separation of 55Co and 58mCo from 54Fe, 58Ni and 57Fe targets

TM1-IR680 peptide for assessment of surgical margin and lymph node metastasis in murine orthotopic model of oral cancer

PET radiometals for antibody labeling

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