Chemical and biological evaluation of scandium(III)-polyaminopolycarboxylate complexes as potential PET agents and radiopharmaceuticals

Huclier‐Markai, Sandrine; Sabatie, A.; Ribet, Solange; Kubíček, Vojtěch; Paris, Michaël; Vidaud, Claude; Hermann, Petr; Cutler, Cathy S.

doi:10.1524/ract.2011.1869

Cited by 33 publications

(53 citation statements)

References 39 publications

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“…[18,20] Stability constants of scandium(III) complexes with these ligands are much higher (4-6 orders of magnitude) than those of lanthanide(III) or gallium(III) complexes. [33,42,43] It is expected, as interaction of such a small hard metal ion with highly charged polycarboxylate ligands is stronger (in comparison with Ln 3 + -complexes, eight donor atoms) and the Sc 3 + ion employs all available donor atoms of the ligands (in comparison with Ga 3 + complexes with six donor atoms).…”

Section: Stability Constants Of the Scandium(iii) Complexesmentioning

confidence: 99%

“…Quantification of complex formation in Sc 3 + -DTPA system was possible by direct integration of the 45 Sc NMR chemical [18] the spectra were re-examined here. They were measured at pH 5 to assure the complete deprotonation of the complexes and formation of the "incage" complex.…”

Section: Sc Nmr Spectroscopymentioning

confidence: 99%

“…Stability constants of only several scandium(III) complexes with polyaminopolyacetate ligands have been published: EDTA (log K ScL 25.0, [28] 23.9 [40] ), DTPA (log K ScL 22.5, [18] 24.5, [40] 26.3 [29] ), and DOTA (log K ScL 22.5 [18] or 27.0 [20] ). Mostly, the values were determined by non-conventional methods and, thus, those for Sc 3 + -DTPA and Sc 3 + -DOTA systems were re-examined here by potentiometry, which is the most common method for stability constant determinations.…”

Section: Stability Constants Of the Scandium(iii) Complexesmentioning

confidence: 99%

“…Such radiopharmaceuticals should be eliminated from the body of the patient unchanged if they do not reach the targeted tissue. The most utilized radioisotope, 18 F, and some others as 13 N, 15 O, or 131 I are non-metallic elements; however, another common isotope, 99m Tc, and most of the emerging isotopes (e.g., 68 Ga, 90 Y, 111 In, 153 Sm, 177 Lu, etc.) are metallic ones.…”

Section: Introductionmentioning

confidence: 99%

“…It has been shown that DOTA derivatives are suitable ligands for scandium radioisotopes. [18][19] Their oligopeptide, [8,11,[20][21][22] antibody, [23] or other [24,25] conjugates have been investigated for complexation of the scandium radionuclides. Surprisingly, only several studies dealing with structure of DTPA or DOTA scandium(III) complexes have been published.…”

Section: Introductionmentioning

confidence: 99%

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Thermodynamic and Kinetic Study of Scandium(III) Complexes of DTPA and DOTA: A Step Toward Scandium Radiopharmaceuticals

Pniok

Kubíček

Havlíčková

et al. 2014

Chemistry A European J

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Diethylenetriamine-N,N,N',N'',N''-pentaacetic acid (DTPA) and 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) scandium(III) complexes were investigated in the solution and solid state. Three (45)Sc NMR spectroscopic references suitable for aqueous solutions were suggested: 0.1 M Sc(ClO4)3 in 1 M aq. HClO4 (δSc =0.0 ppm), 0.1 M ScCl3 in 1 M aq. HCl (δSc =1.75 ppm) and 0.01 M [Sc(ox)4](5-) (ox(2-) = oxalato) in 1 M aq. K2C2O4 (δSc =8.31 ppm). In solution, [Sc(dtpa)](2-) complex (δSc = 83 ppm, Δν = 770 Hz) has a rather symmetric ligand field unlike highly unsymmetrical donor atom arrangement in [Sc(dota)](-) anion (δSc = 100 ppm, Δν = 4300 Hz). The solid-state structure of K8[Sc2(ox)7]⋅13 H2O contains two [Sc(ox)3](3-) units bridged by twice "side-on" coordinated oxalate anion with Sc(3+) ion in a dodecahedral O8 arrangement. Structures of [Sc(dtpa)](2-) and [Sc(dota)](-) in [(Hguanidine)]2[Sc(dtpa)]⋅3 H2O and K[Sc(dota)][H6 dota]Cl2⋅4 H2O, respectively, are analogous to those of trivalent lanthanide complexes with the same ligands. The [Sc(dota)](-) unit exhibits twisted square-antiprismatic arrangement without an axial ligand (TSA' isomer) and [Sc(dota)](-) and (H6 dota)(2+) units are bridged by a K(+) cation. A surprisingly high value of the last DOTA dissociation constant (pKa =12.9) was determined by potentiometry and confirmed by using NMR spectroscopy. Stability constants of scandium(III) complexes (log KScL 27.43 and 30.79 for DTPA and DOTA, respectively) were determined from potentiometric and (45)Sc NMR spectroscopic data. Both complexes are fully formed even below pH 2. Complexation of DOTA with the Sc(3+) ion is much faster than with trivalent lanthanides. Proton-assisted decomplexation of the [Sc(dota)](-) complex (τ1/2 =45 h; 1 M aq. HCl, 25 °C) is much slower than that for [Ln(dota)](-) complexes. Therefore, DOTA and its derivatives seem to be very suitable ligands for scandium radioisotopes.

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Section: Stability Constants Of the Scandium(iii) Complexesmentioning

confidence: 99%

Section: Sc Nmr Spectroscopymentioning

confidence: 99%

Section: Stability Constants Of the Scandium(iii) Complexesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Thermodynamic and Kinetic Study of Scandium(III) Complexes of DTPA and DOTA: A Step Toward Scandium Radiopharmaceuticals

Pniok

Kubíček

Havlíčková

et al. 2014

Chemistry A European J

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Coordination Chemistry and Ligand Design in the Development of Metal Based Radiopharmaceuticals

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Ligand Design in Medicinal Inorganic Chemistry

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Emerging Therapeutic Radiopharmaceuticals and Their Theranostic Pairs

Carbo-Bague

Ramogida

2021

Encyclopedia of Inorganic and Bioinorganic Chemistry

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Nuclear medicine is a rapidly evolving multidisciplinary research field that has been intensively investigated in the past decades. The successful clinical application of various metal‐based radiopharmaceuticals for cancer imaging and therapy is based on the modular assembly of the drug complex through the popular bifunctional chelate (BFC) strategy. In targeted radionuclide therapy (TRT), potent radiation is selectively delivered to the cancer cells using radiopharmaceuticals that incorporate therapeutic radiometals which emit α ‐particles, β − ‐particles, or Meitner–Auger electrons (MAEs). Radiotheranostics is an emerging concept that connects nuclear imaging (via positron emission tomography (PET) or single‐photon emission computed tomography (SPECT)) and therapy for personalized cancer diagnosis and treatment. This article outlines the fundamentals of radiopharmaceutical design and radiotheranostics and presents a general description of the therapeutic emissions accompanied by literature examples of the most promising radionuclides; 212 Pb, 213 Bi, 225 Ac, 227 Th, and 149 Tb for α therapy; 47 Sc, 67 Cu, 77 As, and 161 Tb for β − therapy; and 119 Sb, 135 La, and 197m/g Hg for MAE therapy. A comparison of the currently used or proposed theranostic pairs of each radiometal is presented.

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Chemical and biological evaluation of scandium(III)-polyaminopolycarboxylate complexes as potential PET agents and radiopharmaceuticals

Abstract: International audienc

Cited by 33 publications

References 39 publications

Thermodynamic and Kinetic Study of Scandium(III) Complexes of DTPA and DOTA: A Step Toward Scandium Radiopharmaceuticals

Thermodynamic and Kinetic Study of Scandium(III) Complexes of DTPA and DOTA: A Step Toward Scandium Radiopharmaceuticals

Coordination Chemistry and Ligand Design in the Development of Metal Based Radiopharmaceuticals

Emerging Therapeutic Radiopharmaceuticals and Their Theranostic Pairs

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