Bisphosphonates as Radiopharmaceuticals: Spotlight on the Development and Clinical Use of DOTAZOL in Diagnostics and Palliative Radionuclide Therapy

Bisphosphonates are therapeutic agents that have been used for almost five decades in the treatment of various bone diseases, such as osteoporosis, Paget disease and prevention of osseous complications in cancer patients. In nuclear medicine, simple bisphosphonates such as Tc-radiolabelled oxidronat...

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Bibliographic Details
Published in:International journal of molecular sciences 2023-12, Vol.25 (1), p.462
Main Authors: Souche, Céleste, Fouillet, Juliette, Rubira, Léa, Donzé, Charlotte, Deshayes, Emmanuel, Fersing, Cyril
Format: Article
Language:English
Subjects:
68Ga
Bisphosphonates
bone metastases
Breast cancer
Cancer
Cancer therapies
Carbon
Chemical Sciences
Chemistry
Denosumab
Disodium pamidronate
DOTAZOL
Fractures
Hydroxyapatite
Hypercalcemia
Life Sciences
Metastasis
Nitrogen
Nuclear medicine
Prostate cancer
Radiation therapy
Radiochemistry
Review
theranostics
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Summary:Bisphosphonates are therapeutic agents that have been used for almost five decades in the treatment of various bone diseases, such as osteoporosis, Paget disease and prevention of osseous complications in cancer patients. In nuclear medicine, simple bisphosphonates such as Tc-radiolabelled oxidronate and medronate remain first-line bone scintigraphic imaging agents for both oncology and non-oncology indications. In line with the growing interest in theranostic molecules, bifunctional bisphosphonates bearing a chelating moiety capable of complexing a variety of radiometals were designed. Among them, DOTA-conjugated zoledronate (DOTAZOL) emerged as an ideal derivative for both PET imaging (when radiolabeled with Ga) and management of bone metastases from various types of cancer (when radiolabeled with Lu). In this context, this report provides an overview of the main medicinal chemistry aspects concerning bisphosphonates, discussing their roles in molecular oncology imaging and targeted radionuclide therapy with a particular focus on bifunctional bisphosphonates. Particular attention is also paid to the development of DOTAZOL, with emphasis on the radiochemistry and quality control aspects of its preparation, before outlining the preclinical and clinical data obtained so far with this radiopharmaceutical candidate.
ISSN:1422-0067
1661-6596
1422-0067
DOI:10.3390/ijms25010462