This review presents results on the pharmacokinetic characteristics of osteotropic radiopharmaceuticals (RP) based on polyaminophosphonic acids labeled with various radionuclides. The greatest number of studies cited in the scientific literature address ethylenediaminetetramethylenephosphonic (EDTMP), propylenediaminetetramethylenephosphonic (PDTMP), diethylenetriaminepentakis(methylphosphonic) (PPA), triethylenetetraminohexamethylenephosphonic (TTHMP), 1,4,7,10-tetraazacyclododecan-1,4,7,10-tetramethylenephosphonic (DOTMP) and other acids. RP based on these have high stability in vitro and in vivo, with selective accumulation in bone tissue, and are excreted mainly via the kidneys. This review also presents data on a wide spectrum of radionuclides used to label the various phosphonic acids. These include radionuclides used in radionuclide diagnosis (99mTc, 68Ga) and radionuclide therapy - γ emitters: 153Sm, 188Re, 177Lu, 170Tm, 166Ho, and others, and α emitters: 227Th, 228Ac, and 212Bi.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 49, No. 7, pp. 3 – 9, July, 2015.
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Tishchenko, V.K., Petriev, V.M. & Skvortsov, V.G. Radiopharmaceuticals Based on Polyaminophosphonic Acids Labeled with α−, β−, and γ-Emitting Radionuclides (Review). Pharm Chem J 49, 425–431 (2015). https://doi.org/10.1007/s11094-015-1299-4
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DOI: https://doi.org/10.1007/s11094-015-1299-4