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Pharmacokinetics in Intact Rats of N,N,N′,N′-Ethylenediaminetetrakis-(Methylenephosphonic Acid) Labeled with Gallium-68

  • MOLECULAR-BIOLOGICAL PROBLEMS OF DRUG DESIGN AND MECHANISM OF DRUG ACTION
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Pharmaceutical Chemistry Journal Aims and scope

Pharmacokinetic studies of the new bone-seeking radiopharmaceutical (RP) 68Ga-labeled N,N,N′,N′-ethylenediaminetetrakis(methylenephosphonic acid) (EDTMP) for PET diagnosis of bone metastases showed that 68Ga-EDTMP accumulated rapidly in bone 1 h after i.v. injection, e.g., up to 3.55 ± 0.20%/g in femur, 2.24 ± 0.13%/g in vertebrae, 2.00 ± 0.21%/g in rib, and 1.81 ± 0.10%/g in skull, was cleared rapidly from blood, and had minimal uptake in internal organs and tissues. Most of the activity was excreted through the urinary tract. Knee joints also had significant 68Ga-EDTMP accumulations. It was found that the bone concentration of 68Ga-EDTMP was significantly greater than that of 68GaCl3 (p < 0.001 – 0.05). The ratios of specific activity in bone to those in organs and tissues (differential accumulation factors, DAFs) were greater than unity at all time points. For example, the maximum femur/blood and femur/muscle ratios were 8.00 ± 1.31 and 43.1 ± 7.4. Thus, 68Ga-EDTMP could be considered a potential RP for PET imaging of bone damage.

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Authors and Affiliations

  1. A. Tsyb Medical Radiological Research Centre – Branch of the National Medical Research Radiological Centre of the Ministry of Health of the Russian Federation (A. Tsyb MRRC), Obninsk, Kaluga Region, Russia

    V. M. Petriev, V. K. Tishchenko, O. A. Smoryzanova & V. G. Skvortsov

  2. National Research Nuclear University MEPhI (Moscow Engineering Physics Institute), Moscow, Russia

    V. M. Petriev

Authors
  1. V. M. Petriev
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  2. V. K. Tishchenko
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  3. O. A. Smoryzanova
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  4. V. G. Skvortsov
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Correspondence to V. M. Petriev.

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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 51, No. 5, pp. 3 – 8, May, 2017.

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Petriev, V.M., Tishchenko, V.K., Smoryzanova, O.A. et al. Pharmacokinetics in Intact Rats of N,N,N′,N′-Ethylenediaminetetrakis-(Methylenephosphonic Acid) Labeled with Gallium-68. Pharm Chem J 51, 331–336 (2017). https://doi.org/10.1007/s11094-017-1608-1

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  • DOI: https://doi.org/10.1007/s11094-017-1608-1

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