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

“…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.…”

“…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.…”

“…In order to exploit these characteristics, effective tumour targeting is very important, therefore modified phosphonates are proposed, for example PEI-MP, to selectively deliver the radionuclide to the site [12] - Fig. 1.…”

“…In this paper, the stability of the complexation of Sn 4+ with physiological ligands was studied. A selection of 11 amino acids was made from the many potential physiological ligands to construct LFER curves [12]. From these LFER's the stability constants of the complexation of Sn 4+ with the remaining amino acids or other blood plasma ligands could be estimated based on the known data for the complexes of Cu 2+ , Pb 2+ and Zn 2+ .…”

Chelating agents for radiolanthanides: Applications to imaging and therapy

“…Both 166 Ho and 153 Sm complexes of the boneseeking ligand APDDMP have been isolated and assessed for stability and biodistribution in baboon animal studies. 55 The studies show that 166 Ho-APDDMP has little liver or bone uptake, but that 153 Sm-APDDMP does have moderate bone uptake.…”