We investigate biodistribution of gallium-labeled hydroxyethylidenediphosphonic acid (68Ga-HEDP) and diethylenetriaminepentakis(methylenephosphonic acid) (68Ga-DTPMP) in intact Wistar rats. It was shown that 68Ga-DTPMP accumulated mainly in the bone tissue providing high femur/blood and femur/muscle ratios and had high stability in vivo. In contrast, 68Ga-HEDP was characterized by low stability and high uptake of radioactivity in blood throughout the study. So 68Ga-DTPMP can be considered as a new prospective radiotracer in oncology for imaging bone tissue metastasis by positron emission tomography.
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Kulikov VA, Belyaeva LE. Metabolic reprogramming of cancer cells. Vestn. Vitebsk. Gos. Med. Univer. 2013;12(2):6-18. Russian.
Petriev VM, Tishchenko VK, Krasikova RN. 18F-FDG and Other Labeled Glucose Derivatives for Use in Radionuclide Diagnosis of Oncological Diseases (Review). Pharm. Chem. J. 2016;50(4):209-220.
Autio A, Virtanen H, Tolvanen T, Liljenbäck H, Oikonen V, Saanijoki T, Siitonen R, Käkelä M, Schüssele A, Teräs M, Roivainen A. Absorption, distribution and excretion of intravenously injected 68Ge/68Ga generator eluate in healthy rats, and estimation of human radiation dosimetry. EJNMMI Res. 2015;5. ID 40. https://doi.org/10.1186/s13550-015-0117-z
Bernstein LR. Mechanisms of therapeutic activity for gallium. Pharmacol. Rev. 1998;50(4):665-682.
Coleman RE. Clinical features of metastatic bone disease and risk of skeletal morbidity. Clin. Cancer Res. 2006;12(20, Pt 2):6243s-6249s.
Coleman RE. Metastatic bone disease: Clinical features, pathophysiology and treatment strategies. Cancer Treat. Rev. 2001;27(3):165-176.
Kawabata H. Transferrin and transferrin receptors update. Free Radic. Biol. Med. 2019;133:46-54.
Lin WY, Lin CP, Yeh SJ, Hsieh BT, Tsai ZT, Ting G, Yen TC, Wang SJ, Knapp FF Jr, Stabin MG. Rhenium-188 hydroxyethylidene diphosphonate: a new generator-produced radiotherapeutic drug of potential value for the treatment of bone metastases. Eur. J. Nucl. Med. 1997;24(6):590-595.
Ogawa K, Saji H. Advances in drug design of radiometalbased imaging agents for bone disorders. Int. J. Mol. Imaging. 2011;2011. ID 537687. https://doi.org/10.1155/2011/537687
Pavlova NN, Thompson CB. The emerging hallmarks of cancer metabolism. Cell Metab. 2016;23(1):27-47.
Rösch F. Past, present and future of 68Ge/68Ga generators. Appl. Radiat. Isot. 2013;76:24-30.
Shiryaeva VK, Petriev VM, Bryukhanova AA, Smoryzanova OA, Skvortsov VG. Comparative analysis of pharmacokinetic characteristics of radiopharmaceuticals based on the monopotassium salt of 1-hydroxyethylidenediphosphonic acid labeled by 99mTc and 188Re. Pharm. Chem. J. 2011;45(6):333-340.
Smith TA. Mammalian hexokinases and their abnormal expression in cancer. Br. J. Biomed. Sci. 2000;57(2):170-178.
Suva LJ, Washam C, Nicholas RW, Griffin RJ. Bone metastasis: mechanisms and therapeutic opportunities. Nat. Rev. Endocrinol. 2011;7(4):208-218.
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Translated from Byulleten’ Eksperimental’noi Biologii i Meditsiny, Vol. 168, No. 12, pp. 739-743, December, 2019
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Tishchenko, V.K., Petriev, V.M., Mikhailovskaya, A.A. et al. Experimental Study of the Biodistribution of New Bone-Seeking Compounds Based on Phosphonic Acids and Gallium-68. Bull Exp Biol Med 168, 777–780 (2020). https://doi.org/10.1007/s10517-020-04800-1
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DOI: https://doi.org/10.1007/s10517-020-04800-1