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Relevance of Palladium to Radiopharmaceutical Development Considering Enhanced Coordination Properties of TE1PA

Pineau, Julie ; Lima, Luís M. P. ; Platas‐Iglesias, Carlos ; Zeevaart, Jan Rijn ; Driver, Cathryn H. S. ; Le Bris, Nathalie ; Tripier, Raphaël

Chemistry : a European journal, 2022-07, Vol.28 (41), p.e202200942-n/a [Periódico revisado por pares]

Germany: Wiley Subscription Services, Inc

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Título:
Relevance of Palladium to Radiopharmaceutical Development Considering Enhanced Coordination Properties of TE1PA
Autor: Pineau, Julie ; Lima, Luís M. P. ; Platas‐Iglesias, Carlos ; Zeevaart, Jan Rijn ; Driver, Cathryn H. S. ; Le Bris, Nathalie ; Tripier, Raphaël
Assuntos: Chemical Sciences ; Chemistry ; Clinical trials ; complexation ; Coordination ; Coordination chemistry ; cyclam ; cyclam monopicolinate ; Medical imaging ; Medicinal Chemistry ; Medicine ; Nuclear medicine ; Nuclides ; Palladium ; palladium(II) ; palladium-109 ; Pharmaceuticals ; Positron emission ; Positron emission tomography ; Radiation therapy ; Radiochemistry ; Radioisotopes ; radiolabeling ; Radiolabelling ; Thermodynamic properties ; Thermodynamics
É parte de: Chemistry : a European journal, 2022-07, Vol.28 (41), p.e202200942-n/a
Notas: ObjectType-Article-1
SourceType-Scholarly Journals-1
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Descrição: The limited use of palladium‐103 and ‐109 radionuclides for molecular radiotherapy is surely due to the lack of appropriate ligands capable of fulfilling all criteria required for application in nuclear medicine. Furthermore, the thermodynamic properties of these complexes in solution remain difficult to establish. The challenge is compounded when considering that radiolabeling of compounds for translation to clinical trials requires fast complexation. Thus, the coordination of Pd(II) and 103/109Pd‐nuclides is a huge challenge in terms of molecular design and physicochemical characterization. Herein, we report a comprehensive study highlighting TE1PA, a monopicolinate cyclam – already established in nuclear imaging with 64Cu‐PET (positron emission tomography) imaging tracers – as a highly relevant chelator for natural Pd and subsequently 109Pd‐nuclide. The structural, thermodynamic, kinetic and radiolabeling studies of Pd(II) with TE1PA, as well as the comparison of this complex with three structurally related derivatives, support palladium‐TE1PA radiopharmaceuticals as leading candidates for targeted nuclear medicine. Radiopharmaceuticals: Since the macrocyclic gold standards used in nuclear medicine are not suitable to Pd(II) coordination, its radioisotopes remain understated for radiopharmaceutical applications. The monopicolinate cyclam TE1PA presented here is a highly relevant chelator for natural and radioactive Pd, opening avenues to enrich the current palette of radiopharmaceuticals for targeted radiotherapy.
Editor: Germany: Wiley Subscription Services, Inc
Idioma: Inglês

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Relevance of Palladium to Radiopharmaceutical Development Considering Enhanced Coordination Properties of TE1PA

Pineau, Julie ; Lima, Luís M. P. ; Platas‐Iglesias, Carlos ; Zeevaart, Jan Rijn ; Driver, Cathryn H. S. ; Le Bris, Nathalie ; Tripier, Raphaël

Germany: Wiley Subscription Services, Inc

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