Abstract
Radiopharmaceuticals (RPs) administered intravenously are included into metabolic pathways of the body via binding to carrier molecules, and carrier kinetics is crucial for achieving a therapeutic or diagnostic effect as a result. In silico modeling the RP transport kinetics is important because quantitative information can be obtained about RP transfer between organs (chambers, or compartments). Folic acid conjugates labeled with 68Ga are among promising agents for diagnostic imaging of malignant neoplasms and rheumatic pathologies. The kinetics of folic acid-based RPs was studied using experimental data obtained in Wistar rat models of inflammation due to various causes. The study confirmed that the amino acid fragment His-Glu-His-Glu introduced in the molecule as part of the [68Ga]Ga-FA-II conjugate significantly reduces the radioactivity uptake in the kidney as opposed to the unmodified analog [68Ga]Ga-FA-I. Alterations in pharmacokinetic parameters observed after administration of the amino acid fragment-modified agent suggest a significant reduction in radiation doses on critical organs and tissues and are expected to promote application of the compounds under study in positron emission tomography imaging of pathological processes.
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Translated by T. Tkacheva
Abbreviations: RP, radiopharmaceutical; JIA, juvenile idiopathic arthritis.
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Lunev, A.S., Lunyova, K.A., Vasilevich, F.I. et al. Kinetic Study of Folate-Based Radiopharmaceuticals Labeled with 68Ga. BIOPHYSICS 67, 1000–1006 (2022). https://doi.org/10.1134/S0006350922060124
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DOI: https://doi.org/10.1134/S0006350922060124