Publication: Pharmacokinetics of Ga-68-NODA-aminoglucose in mice with Ehrlich carcinoma
Дата
2020
Авторы
Tishchenko, V. K.
Mikhailovskaya, A. A.
Fedorova, A. V.
Stepchenkova, E. D.
Petriev, V. M.
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© 2020 National Medical Research Radiological Centre of the Ministry of Health of the Russian Federation. All rights reserved.The clinical application of Positron Emission Tomography (PET) is growing in Russia. To increase the accessibility of PET-procedures for the general public, the development of cost-effective radio-tracers has become of particular importance. The paper presents results of the study of pharmaco-kinetic properties of the new compound contained based on NODA-aminoglucose and generate ra-dionuclide gallium-68 (68Ga-NODA-AG). Intact outbred mice and mice with subcutaneously inocu-lated Ehrlich carcinoma were taken in the study. Concentration of 68Ga-NODA-AG was measured by direct radiometry. The same method was used for calculation of biological and effective half-lives of the radiopharmaceutical. Binding efficacy of 68Ga with NODA-AG was above 95%. The content of radiochemical impurities was less than 5%. Specific activity of 68Ga-NODA-AG in the tumor re-duced from 3.19 %/g in 5 minutes after the radiotracer administration to 0.93 %/g, 0.34 %/g and 0.31 %/g in 1, 2, 3 hours respectively. Because an increased amount of radioactivity is accumulated in the tumor as compared with healthy tissues and organs the rate of 68Ga-NODA-AG clearance from the tumor tissue was relatively low. The compound was cleared by renal route. It should be stressed that 68Ga-NODA-AG concentration in the brain and the heart was low. Accumulation of ra-dioactivity in tumor-bearing mice was lower than in intact animals mainly at early stages of the study. Biological and effective half-lives of the radiopharmaceutical in all organs and tissues except for the brain were higher in tumor-bearing mice than in intact animals. The obtained results allow making the following conclusion: the pharmacokinetic properties of 68Ga-NODA-AG are optimal for diagnostic radiopharmaceuticals.
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Pharmacokinetics of Ga-68-NODA-aminoglucose in mice with Ehrlich carcinoma / Tishchenko, V.K. [et al.] // Radiation and Risk. - 2020. - 29. - № 3. - P. 60-70. - 10.21870/0131-3878-2020-29-3-60-70