Pharmacokinetics in Intact Rats of N,N,N′,N′-Ethylenediaminetetrakis-(Methylenephosphonic Acid) Labeled with Gallium-68
| Autor: | O. A. Smoryzanova, V. G. Skvortsov, V. K. Tishchenko, V. M. Petriev |
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| Rok vydání: | 2017 |
| Předmět: |
Pharmacology
EDTMP medicine.medical_specialty Urinary system Pet imaging 01 natural sciences 0104 chemical sciences 010404 medicinal & biomolecular chemistry 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Endocrinology chemistry Pharmacokinetics 030220 oncology & carcinogenesis Internal medicine Drug Discovery medicine Specific activity Femur Bone damage Clearance |
| Zdroj: | Pharmaceutical Chemistry Journal. 51:331-336 |
| ISSN: | 1573-9031 0091-150X |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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