Complexation studies with 90Y from a novel 90Sr-90Y generator

Venkatesh, Meera; Pandey, Amit Kumar; Dhami, P.S.; Kannan, Rangasayee; Achuthan, P. V.; Chitnis, R. R.; Gopalakrishnan, V.; Banerjee, Sharmila; Samuel, Grace; Pillai, M.R.A.; Ramanujam, A.

doi:10.1524/ract.2001.89.6.413

Cited by 32 publications

(9 citation statements)

References 17 publications

(22 reference statements)

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“…This is confirmed when comparing this result with those reported by Venkatesh for [ 90 Y(DOTA)], which showed a stability of ≥90% at 24 h under similar conditions. 35 This result is also comparable to [ 90 Y(DTPA)]-IgG, where a dissociation of 8−9% per day in serum at 37 °C was measured. 36 ■ CONCLUSIONS…”

Section: ■ Results and Discussionsupporting

confidence: 71%

Pyclen Tri-n-butylphosphonate Ester as Potential Chelator for Targeted Radiotherapy: From Yttrium(III) Complexation to ⁹⁰Y Radiolabeling

et al. 2016

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The Y(3+) complex of PCTMB, the tri-n-butyl phosphonate ester of pyclen (3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-triene), was synthesized as well as its Ho(3+) and Lu(3+) analogues. X-ray diffraction analyses revealed isomorphous dimeric M2(PCTMB)2·9H2O (M = Y, Ho, Lu) structures that crystallize in the centrosymmetric P1̅ triclinic space group. (1)H NMR and UV studies in aqueous solutions indicated that Y(3+) complexation is fast, being quantitative in 167 min at pH 3.8 and in 13 min at pH 5.5 (25 °C, acetate buffer, I = 0.150 M, [Y(3+)] = [PCTMB] = 0.2 mM). (1)H NMR DOSY and photon correlation spectroscopy experiments evidenced the formation of aggregates in chloroform with a bimodal distribution that changes slightly with concentration (11-24 and 240-258 nm). The behavior of the acid-assisted dissociation of the complex of Y(3+) with PCTMB was studied under pseudo-first-order conditions, and the half-life of the [Y(PCTMB)] complex in 0.5 M HCl at 25 °C was found to be 37 min, a value that decreases to 2.6 min in 5 M HCl. The Y(3+) complex of PCTMB is thermodynamically very stable, with a stability constant of log KY-PCTMB = 19.49 and pY = 16.7 measured by potentiometry. (90)Y complexation studies revealed fast radiolabeling kinetics; optimal radiolabeling conditions were obtained for (90)Y in acetate medium, PCTMB at 10(-4) to 10(-2) M in acetate buffer pH = 4.75, 15 min at 45-60 °C. In vitro stability studies in human serum showed that [(90)Y(PCTMB)] is quite stable, with about 90% of the activity still in the form of the radiotracer at 24 h and 80% from 48 h to 72 h. A comparison with other ligands such as PCTA, DOTA, and DTPA already used for in vivo application shows that [(90)Y(PCTMB)] is an interesting lipophilic and neutral analogue of these reference chelates for therapeutic applications in aqueous and nonaqueous media.

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Section: ■ Results and Discussionsupporting

confidence: 71%

Pyclen Tri-n-butylphosphonate Ester as Potential Chelator for Targeted Radiotherapy: From Yttrium(III) Complexation to ⁹⁰Y Radiolabeling

et al. 2016

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“…Yttrium possesses a particularly interesting isotope, 90 Y, which is a pure β – emitter with a half-life of 64.2 h and a decay energy of 2.28 MeV. Yttrium-90 disintegrates into the stable 90 Zr isotope and can be produced both by neutron activation from stable 89 Y or from a 90 Sr/ 90 Y generator . The interest in yttrium(III) is also justified by the existence of the β + emitter 86 Y suitable for PET imaging.…”

Section: Introductionmentioning

confidence: 99%

Stable and Inert Yttrium(III) Complexes with Pyclen-Based Ligands Bearing Pendant Picolinate Arms: Toward New Pharmaceuticals for β-Radiotherapy

et al. 2018

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We report the synthesis of two azaligands based on the pyclen macrocyclic platform containing two picolinate and one acetate pendant arms. The two ligands differ in the relative positions of the pendant functions, which are arranged either in a symmetrical (L3) or nonsymmetrical (L4) fashion. The complexation properties of the ligands toward Y and Y were investigated to assess their potential as chelating units for radiopharmaceutical applications. The X-ray structures of the YL3 and YL4 complexes show nonadentate binding of the ligand to the metal ions. A multinuclear H,C, and Y NMR study shows that the complexes present a structure in solution similar to that observed in the solid state. The two complexes present very high thermodynamic stability constants (log K = 23.36(2) and 23.07(2) for YL3 and YL4, respectively). The complexes also show a remarkable inertness with respect to their proton-assisted dissociation, especially YL4. Y radiolabeling was proved to be efficient under mild conditions. TheYL3 and YL4 radiochelates were found to be more stable thanY(DOTA).

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“…The 90 Sr activity present at the solvent front was then compared to the total applied activity to obtain the radionuclidic impurity levels. Radiochemical purity was determined by paper chromatography using saline as the mobile phase and by paper electrophoresis [44]. Chemical purity was determined by Inductively Coupled Plasma Atomic Emission Spectroscopy (ICP-ES JY-238, Emission Horiba Group, France) analysis of the decayed sample.…”

Section: Methodsmentioning

confidence: 99%

Utilization of a novel electrochemical ⁹⁰Sr/⁹⁰Y generator for the preparation of ⁹⁰Y-labeled RGD peptide dimer in clinically relevant dose

et al. 2014

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The work reported in this paper provides a systematic study towards the development of an optimized strategy for preparation of a clinically relevant dosefor in vivo targeted therapy utilizing 90 Y obtained from a novel electrochemical 90 Sr/ 90 Y generator. The performance of the generator was evaluated to ensure its suitability for providing 90 Y in adequate quantity and purity required for formulation of clinically relevant dose for PRRT. 90 Y-DOTA-(RGD) 2 was synthesized in high yield (86.2 ± 2.5%) and radiochemical purity (98.4 ± 0.5%) using clinically relevant dose (∼3.8 GBq) of 90 Y. In vitro stability studies revealed that the radiolabeled conjugate retained its radiochemical purity in normal saline and human serum. Preliminary biodistribution studies carried out in C57/BL6 mice bearing melanoma tumors showed that the preparation exhibited significant tumor uptake (5.30 ± 0.78% of injected activity at 30 min post-injection) with good tumor to background ratio. The optimized radiolabeling protocol seems to be an attractive strategy which is largely viewed as a springboard to realize scope of developing 90 Y labeled cyclic RGD peptides for targeted therapy of tumors overexpressing integrin-3 receptors.

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Complexation studies with ⁹⁰Y from a novel ⁹⁰Sr-⁹⁰Y generator

Cited by 32 publications

References 17 publications

Pyclen Tri-n-butylphosphonate Ester as Potential Chelator for Targeted Radiotherapy: From Yttrium(III) Complexation to ⁹⁰Y Radiolabeling

Pyclen Tri-n-butylphosphonate Ester as Potential Chelator for Targeted Radiotherapy: From Yttrium(III) Complexation to ⁹⁰Y Radiolabeling

Stable and Inert Yttrium(III) Complexes with Pyclen-Based Ligands Bearing Pendant Picolinate Arms: Toward New Pharmaceuticals for β-Radiotherapy

Utilization of a novel electrochemical ⁹⁰Sr/⁹⁰Y generator for the preparation of ⁹⁰Y-labeled RGD peptide dimer in clinically relevant dose

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Complexation studies with 90Y from a novel 90Sr-90Y generator

Cited by 32 publications

References 17 publications

Pyclen Tri-n-butylphosphonate Ester as Potential Chelator for Targeted Radiotherapy: From Yttrium(III) Complexation to 90Y Radiolabeling

Pyclen Tri-n-butylphosphonate Ester as Potential Chelator for Targeted Radiotherapy: From Yttrium(III) Complexation to 90Y Radiolabeling

Stable and Inert Yttrium(III) Complexes with Pyclen-Based Ligands Bearing Pendant Picolinate Arms: Toward New Pharmaceuticals for β-Radiotherapy

Utilization of a novel electrochemical 90Sr/90Y generator for the preparation of 90Y-labeled RGD peptide dimer in clinically relevant dose

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Complexation studies with ⁹⁰Y from a novel ⁹⁰Sr-⁹⁰Y generator

Pyclen Tri-n-butylphosphonate Ester as Potential Chelator for Targeted Radiotherapy: From Yttrium(III) Complexation to ⁹⁰Y Radiolabeling

Pyclen Tri-n-butylphosphonate Ester as Potential Chelator for Targeted Radiotherapy: From Yttrium(III) Complexation to ⁹⁰Y Radiolabeling

Utilization of a novel electrochemical ⁹⁰Sr/⁹⁰Y generator for the preparation of ⁹⁰Y-labeled RGD peptide dimer in clinically relevant dose