| Added by | JPPOUGET |
|---|---|
| Group name | EquipeJPP |
| Item Type | Journal Article |
| Title | Bisphosphonates as Radiopharmaceuticals: Spotlight on the Development and Clinical Use of DOTAZOL in Diagnostics and Palliative Radionuclide Therapy |
| Creator | Souche et al. |
| Author | Céleste Souche |
| Author | Juliette Fouillet |
| Author | Léa Rubira |
| Author | Charlotte Donzé |
| Author | Emmanuel Deshayes |
| Author | Cyril Fersing |
| Abstract | 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 99mTc-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 68Ga) and management of bone metastases from various types of cancer (when radiolabeled with 177Lu). 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. |
| Publication | International Journal of Molecular Sciences |
| Volume | 25 |
| Issue | 1 |
| Pages | 462 |
| Date | 2023-12-29 |
| Journal Abbr | Int J Mol Sci |
| Language | eng |
| DOI | 10.3390/ijms25010462 |
| ISSN | 1422-0067 |
| Short Title | Bisphosphonates as Radiopharmaceuticals |
| Library Catalog | PubMed |
| Extra | PMID: 38203632 PMCID: PMC10779041 |
| Tags | 177Lu, 68Ga, Adenocarcinoma, bisphosphonates, bone metastases, Diphosphonates, DOTAZOL, Humans, nuclear medicine, original, Radioisotopes, Radiopharmaceuticals, Scientific, theranostics, Zoledronic Acid |
| Date Added | 2024/12/07 - 07:57:50 |
| Date Modified | 2024/12/15 - 11:45:36 |
| Notes and Attachments | Full Text (Attachment) PubMed entry (Attachment) PubMed entry (Attachment) PubMed entry (Attachment) PubMed entry (Attachment) |
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