Comparison of the predicted in vivo behaviour of the Sn(II)–APDDMP complex and the results as studied in a rodent model

Zeevaart, Jan Rijn; Jansen, David R.; Botelho, Maria Filomena; Abrunhosa, Antero; Metello, Luiz; Kolář, Z.; Krijger, Gerard C.; Louw, Werner; Dormehl, I. C.

doi:10.1016/j.jinorgbio.2004.06.004

Cited by 9 publications

(10 citation statements)

References 16 publications

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“…Indeed, this is what we have demonstrated in this study, although the excretion observed was not as rapid as that of other phosphonate-based radiopharmaceuticals reported previously [24].…”

Section: Discussionsupporting

confidence: 81%

Biodistribution and Pharmacokinetics of I-131 Labelled 4- Iodophenylacetic Acid

Zeevaart

Szűcs²,

Pulker³

et al. 2012

CRP

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Phenylacetate has been reported to have a potent anti-proliferative and anti-differentiating effect in haematological malignancies and in solid tumours at non-toxic concentrations. This study is a preliminary investigation of 131 Iradiolabelled 4-iodophenylacetic acid as a potential radiopharmaceutical equivalent. Radiolabelling by isotope exchange gave a radiochemical yield of 53 ± 6 %, and a radiochemical purity of 97.8 ± 1.2 %, as qualified by was recorded with a tumour to background ratio of 2. As the blood pool still contains high levels of activity after 5 h in mice, increased tumour uptake may occur at later time points, which might warrant further investigation.

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“…Indeed, this is what we have demonstrated in this study, although the excretion observed was not as rapid as that of other phosphonate-based radiopharmaceuticals reported previously [24].…”

Section: Discussionsupporting

confidence: 81%

Biodistribution and Pharmacokinetics of I-131 Labelled 4- Iodophenylacetic Acid

Zeevaart

Szűcs²,

Pulker³

et al. 2012

CRP

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“…The difference between formation constants obtained at 25.0°C and at 37.0°C is negligible, as demonstrated by Zeevaart et al [10,11] in their comparison of blood plasma model predictions with the biodistribution in rodents, for N, N-dimethylenephosphonate-1-hydroxy-3-aminopropylidenediphosphonate (APDDMP) as complexed with [ 117m Sn]Sn 2+ . Furthermore, a temperature of 25.0°C is easier to maintain constant and minimizes evaporation and condensation within the reaction vessel, which could affect the concentration of the titre.…”

Section: Reagents and Apparatusmentioning

confidence: 90%

“…3-amino-1-hydroxypropylidene-1,1-diphosphonate (APD) [6,7] and etidronate, 1-hydroxyethylene-diphosphonate (HEDP) [8]. Novel radiopharmaceuticals for the palliation of bone pain have been proposed, which comprises of radiolabelled tin, namely [ 117m Sn]Sn(II) or [ 117m Sn]Sn(IV) [9][10][11]. 117m Sn decays by the emission of conversion electrons and a photon (159 keV, 86.4%), with a half life of 13.6 days.…”

Section: Introductionmentioning

confidence: 99%

Blood plasma model predictions for the proposed bone-seeking radiopharmaceutical [117mSn]Sn(IV)-N,N′,N′-trimethylenephosphonate-poly(ethyleneimine)

Jansen

Krijger

Wagener

et al. 2009

Journal of Inorganic Biochemistry

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“…Our group has recorded some success in using a blood plasma model in predicting and describing potential bone-seeking agents (bisphosphonates) [5][6][7] as opposed to a trial-and-error approach. Most of the agents screened by this in vitro/in silico technique were not found to have potential and drawbacks were indicated.…”

Section: Although 99mmentioning

confidence: 99%

“…This is a well described suite of programs [16] and its use to predict the in vivo behaviour illustrated in several earlier papers [5][6][7] and therefore no detail of this approach is given here. Briefly, the ECCLES formation constant database was updated to include formation constants for the biguanide-type ligands and DMSA with the blood plasma metal ions Ca(II), Mg(II), Zn(II) that were established previously and published elsewhere [11].…”

Section: Blood Plasma Modellingmentioning

confidence: 99%

99mTc-labelled biguanide derivatives: chemical speciation modelling thereof and evaluation in vervets

Zeevaart

Wagener

Neves³

et al. 2009

J Radioanal Nucl Chem

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99mTc-DMSA (dimercaptosuccinic acid) is known to be a safe and effective agent for static renal imaging. However, it has a long uptake time which is a limiting factor in diagnostic procedures and also leads to a relatively high radiation dose being administered to patients. There is a constant search for possible new renal imaging agents with a good resolution, kidney/liver contrast and low radiation dose to all organs. A series of biguanide derivatives (potential as noninsulin-dependent diabetes mellitus agents) labelled with 99m Tc were investigated as potential alternative kidney-imaging agents on theoretical grounds (in silico) and their biodistribution (in vivo) verified in a limited number of animal experiments. Such a dual approach has the benefit that it reduces the number of animal experiments needed to evaluate a potential radiopharmaceutical. The blood plasma model shows little or no complexation of the biguanide type ligands by the metal ions in blood plasma. It was therefore expected that these ligands will clear rapidly through the kidneys and liver (increased lipophilicity). These predictions were verified by studies on single vervets comparing them with Tc-CBIG (carboxylbiguanide) has a very fast kidney clearance, which will reduce the dose to organs (as experienced for 99m Tc-DMSA), although it's potential as a kidney agent is limited by its gallbladder uptake.

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Comparison of the predicted in vivo behaviour of the Sn(II)–APDDMP complex and the results as studied in a rodent model

Cited by 9 publications

References 16 publications

Biodistribution and Pharmacokinetics of I-131 Labelled 4- Iodophenylacetic Acid

Biodistribution and Pharmacokinetics of I-131 Labelled 4- Iodophenylacetic Acid

Blood plasma model predictions for the proposed bone-seeking radiopharmaceutical [117mSn]Sn(IV)-N,N′,N′-trimethylenephosphonate-poly(ethyleneimine)

99mTc-labelled biguanide derivatives: chemical speciation modelling thereof and evaluation in vervets

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