A Comparative Study of the Pharmacokinetics of Bis- and Pentaphosphonic Acids Labeled with Gallium-68 in Rats with Exper
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Bulletin of Experimental Biology and Medicine, Vol. 169, No. 5, September, 2020
PHARMACOLOGY AND TOXICOLOGY A Comparative Study of the Pharmacokinetics of Bisand Pentaphosphonic Acids Labeled with Gallium-68 in Rats with Experimental Model of Bone Callus V. K. Tishchenko1,2, V. M. Petriev1,2, K. A. Kuzenkova1, P. V. Shegai1, S. A. Ivanov1, and A. D. Kaprin1
Translated from Byulleten’ Eksperimental’noi Biologii i Meditsiny, Vol. 169, No. 5, pp. 573-577, May, 2020 Original article submitted February 4, 2020 We analyzed biodistribution of 68Ga-labeled hydroxyethylidenediphosphonic acid (68GaHEDP) and diethylenetriaminepentakis(methylenephosphonic acid) (68Ga-DTPMP) in Wistar rats with experimental model of bone callus. It was shown that the content of 68Ga-DTPMP and 68Ga-HEDP in bone callus was ~1.5-fold higher than in intact femur. 68Ga-DTPMP was characterized by higher stability in vivo, higher uptake in the bone tissue, and lower uptake in others visceral organs in comparison with 68Ga-HEDP. Thus, 68Ga-DTPMP had more suitable pharmacokinetic properties than 68Ga-HEDP. Key Words: gallium-68; diethylenetriaminepentakis(methylenephosphonic acid); hydroxyethylidenediphosphonic acid; bone callus Skeletal metastases accompany many cancer diseases in advanced stage, in particular, breast cancer, prostate cancer, thyroid cancer, as well as lung and kidney cancer [8]. Bone metastases cause bone pain syndrome, are associated with the risk of pathological fractures, and decrease patient’s quality of life and lifespan. Early and accurate diagnosis of skeletal metastases largely determines the approaches and outcome of therapy. Bone scintigraphy with 99mTc-phosphonates is the main diagnostic method for bone metastases [13]. Phosphonates are characterized by high affinity to hydroxyapatite, the main inorganic compound of the bone tissue, and accumulate prominently in metastatic lesions. Positron emission tomography (PET) is one of the most precise and highly sensitive diagnostic method of nuclear medicine. For visualization bone metasNational Medical Research Center of Radiology, Ministry of Health of the Russian Federation, Obninsk; 2National Research Nuclear University MEPhI (Moscow Engineering Physics Institute), Moscow, Russia. Address for correspondence: [email protected]. V. K. Tishchenko 1
tases by PET, 18F-based radiopharmaceuticals (RP) 2-18F-fluorine-2-deoxy-D-glucose (18F-FDG) and 18Fsodium fluoride (18F-NaF) are currently used. A substantial drawback of these RP is the need in special high-technology equipment, medical cyclotron, in the hospital or nearby due to short half-life of the isotope (Т1/2=110 min). High operational costs of cyclotron and the need equipment for automatic synthesis of RP also increase the costs of both the clinical dose of RP and the diagnostic procedure [2]. Generator-based 68Ga is an alternative radionuclide for PET studies. It has appropriate nuclear and physic properties (Т1/2=68 min, β+=89%, E+βmax=1.9 MeV) and can be obtained in cationic form 68Ga3+ from 68Ge/68Ga generator dire
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