177Lu-DOTA-IBA Therapy in Prostate Cancer With Bone Metastases

Li, Hongmei; Xu, Tingting; Hua, Qiao; Wang, Li; Chen, Yue

doi:10.1097/rlu.0000000000004717

Cited by 7 publications

(2 citation statements)

References 12 publications

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“…The highly promising effects of this DOTA-bisphosphonate, radiolabeled with either 68 Ga for PET imaging or 177 Lu for TRT, should be confirmed in a larger population but already suggest the theranostic potential of this molecule. Several case reports support these data [ 166 ], some even reporting the efficacy of DOTA-IBA radiolabeled with alpha emitter actinium-225 [ 167 ].…”

Section: Bisphosphonates: From Conventional Drugs To Radiopharmaceuti...mentioning

confidence: 90%

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

Souche,

Fouillet,

Rubira

et al. 2023

IJMS

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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.

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Section: Bisphosphonates: From Conventional Drugs To Radiopharmaceuti...mentioning

confidence: 90%

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

Souche,

Fouillet,

Rubira

et al. 2023

IJMS

View full text Add to dashboard Cite

show abstract

“…In our case, after treatment, the bone metastasis lesions showed an increase in bone density, and the patient’s painless state remained stable. DOTA-IBA is new a precursor targeting bone metastasis, which can be used for radionuclide labeling with 68 Ga, 177 Lu, and 225 Ac for the diagnosis or treatment of bone metastasis 1–4,10,11 . Our case encourages 177 Lu-DOTA-IBA as a promising therapeutic option in patients with bone metastasis of breast cancer, but more studies and experiments are needed.…”

mentioning

confidence: 82%