Abstract
DOTA-zoledronate was designed to image oseogenic activity in bone.
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Chemical name and alternative names | Chemical structure |
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2,2′,2″-(10-(2-((2-(1-(2-hydroxy-2,2-diphosphono-ethyl)-1H-imidazol-4-yl)ethyl)-amino)-2-oxoethyl)-1,4,7,10-tetraazacyclo-dodecane-1,4,7-triyl)triacetic acid DOTA-ZOL; DOTAZOL |
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Route of Synthesis
Chelation of generator produced 68Ga-chloride with DOTA-zoledronate in acetate buffer at elevated temperature, followed by cartridge purification (Meckel et al. 2017).
Normal Biodistribution and Excretion
High accumulation is seen in the skeleton as biological target and kidneys and bladder as organs of excretion. Faint accumulation is seen in liver, spleen, and salivary glands. Activity is seen in the renal parenchyma within 2.5 min of injection, but renal clearance is rapid and only minimal activity is evident at 45 min (Khawar et al. 2019).
Activity Administered
150 MBq.
Radiation Dosimetry
Effective dose equivalent (mSv/MBq): 0.017 (2.6 mSv/150 MBq).
Organ doses (mGy/MBq): urinary bladder wall, 0.37; osteogenic cells, 0.040; kidneys, 0.031 (Khawar et al. 2019).
Patient Preparation
The patient should be well hydrated to reduce the radiation dose to the kidneys and bladder.
Clinical Utility
It is anticipated that utility will be similar to 18F-fluoride (though with much reduced radiation dose) and the 99mTc diphosphonate bone scan agents. In particular, may be useful prior to palliative therapy with 177Lu- or 225Ac-DOTA-ZOL (Meisenheimer et al. 2020).
Further Reading
Khawar A, Eppard E, Roesch F, et al. Preliminary results of biodistribution and dosimetric analysis of [68Ga]Ga-DOTAZOL: a new zoledronate-based bisphosphonate for PET/CT diagnosis of bone diseases. Ann Nucl Med. 2019;33:404–13.
Meckel M, Bergmann R, Miederer M, et al. Bone targeting compounds for radiotherapy and imaging: *me(III)-DOTA conjugates of bisphosphonic acid, pamidronic acid and zoledronic acid. EJNMMI Radiopharm Chem. 2017;1:14.
Meisenheimer M, Kürpig S, Essler M, et al. DOTA-ZOL: a promising tool in diagnosis and palliative therapy of bone metastasis–challenges and critical points in implementation into clinical routine. Molecules. 2020;25:2988.
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Ballinger, J.R. (2022). 68Ga-DOTA-Zoledronate. In: PET Radiopharmaceuticals. Clinicians’ Guides to Radionuclide Hybrid Imaging(). Springer, Cham. https://doi.org/10.1007/978-3-031-10271-4_29
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DOI: https://doi.org/10.1007/978-3-031-10271-4_29
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