Convenient preparation of 68Ga-based PET-radiopharmaceuticals at room temperature

Bioconjugate Chemistry
Irina VelikyanBengt Långström

Abstract

A straightforward labeling using generator produced positron emitting (68)Ga, which provides high quality images, may result in kit type production of PET radiopharmaceuticals and make PET examinations possible also at centers lacking accelerators. The introduction of macrocyclic bifunctional chelators that would provide fast (68)Ga-complexation at room temperature would simplify even further tracer preparation and open wide possibilities for (68)Ga-labeling of fragile and potent macromolecules. Gallium-68 has the potential to facilitate development of clinically practical PET and to promote PET technique for individualized medicine. The macrocyclic chelator, 1,4,7-triazacyclononanetriacetic acid (NOTA), and its derivative coupled to an eight amino acid residue peptide (NODAGA-TATE, [NODAGA (0), Tyr(3)]Octreotate) were labeled with (68)Ge/(68)Ga-generator produced positron emitting (68)Ga. Formation kinetics of (68)Ga-NOTA was studied as a function of pH and formation kinetics of (68)Ga-NODAGA-TATE was studied as a function of the bioconjugate concentration. The nearly quantitative radioactivity incorporation (RAI>95%) for (68)Ga-NOTA was achieved within less than 10 min at room temperature and pH 3.5. The concentrations of NOD...Continue Reading

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Citations

May 30, 2008·European Journal of Nuclear Medicine and Molecular Imaging·Matthias EderMichael Eisenhut
Nov 17, 2009·European Journal of Nuclear Medicine and Molecular Imaging·Jörg KotzerkeGerd Wunderlich
Mar 6, 2012·European Journal of Nuclear Medicine and Molecular Imaging·Clemens DecristoforoAlfons Verbruggen
Jan 8, 2009·Bioconjugate Chemistry·Tapan K Nayak, Martin W Brechbiel
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