Evaluation of Safety and Dosimetry of <sup>177</sup>Lu-DOTA-ZOL for Therapy of Bone Metastases

Fernández, Ramón Fernández-Guerra; Eppard, Elisabeth; Lehnert, Wencke; Jiménez-Franco, Luis David; Soza‐Ried, Cristian; Ceballos, Matias; Ribbeck, Jessica; Kluge, Andreas; Rösch, Frank; Meckel, Marian; Zhernosekov, Konstantin; Kramer, Vasko; Amaral, Horacio

doi:10.2967/jnumed.120.255851

Cited by 24 publications

(21 citation statements)

References 34 publications

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“…These preliminary data were further confirmed by Fernandez and collaborators, who evaluated the safety and dosimetry of a single dose administration of 177 Lu-DOTA ZOL in 9 patients with bone metastases from mCRPC [20]. The authors found a favorable therapeutic index for the radiocompound, with average absorbed doses in skeletal metastases, kidneys, red bone marrow, and bone surfaces of 4.21, 0.17, 0.36 and 1.19 Gy/GBq, respectively.…”

Section: Radiolabeled Zolendronic Acidmentioning

confidence: 70%

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Prognostic and Theranostic Applications of Positron Emission Tomography for a Personalized Approach to Metastatic Castration-Resistant Prostate Cancer

Filippi

Frantellizzi

Chiaravalloti

et al. 2021

IJMS

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Metastatic castration-resistant prostate cancer (mCRPC) represents a condition of progressive disease in spite of androgen deprivation therapy (ADT), with a broad spectrum of manifestations ranging from no symptoms to severe debilitation due to bone or visceral metastatization. The management of mCRPC has been profoundly modified by introducing novel therapeutic tools such as antiandrogen drugs (i.e., abiraterone acetate and enzalutamide), immunotherapy through sipuleucel-T, and targeted alpha therapy (TAT). This variety of approaches calls for unmet need of biomarkers suitable for patients’ pre-treatment selection and prognostic stratification. In this scenario, imaging with positron emission computed tomography (PET/CT) presents great and still unexplored potential to detect specific molecular and metabolic signatures, some of whom, such as the prostate specific membrane antigen (PSMA), can also be exploited as therapeutic targets, thus combining diagnosis and therapy in the so-called “theranostic” approach. In this review, we performed a web-based and desktop literature research to investigate the prognostic and theranostic potential of several PET imaging probes, such as 18F-FDG, 18F-choline and 68Ga-PSMA-11, also covering the emerging tracers still in a pre-clinical phase (e.g., PARP-inhibitors’ analogs and the radioligands binding to gastrin releasing peptide receptors/GRPR), highlighting their potential for defining personalized care pathways in mCRPC

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Section: Radiolabeled Zolendronic Acidmentioning

confidence: 70%

“…Fernandez et al [20] Prospective, single-center 177 Lu-DOTA ZOL Osteoclastic bone resorption 177 Lu-DOTA ZOL is safe and presents a favorable therapeutic index compared to other radiopharmaceuticals applied for the management of bone metastases.…”

Section: Authors Year Type Of Study Radiotracer Target Commentmentioning

confidence: 99%

Prognostic and Theranostic Applications of Positron Emission Tomography for a Personalized Approach to Metastatic Castration-Resistant Prostate Cancer

Filippi

Frantellizzi

Chiaravalloti

et al. 2021

IJMS

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“…58 The comparison with other bis( phosphonate) bearing macrocycles, which were used as carriers of various metallic radioisotopes (e.g. 68 Ga, 177 Lu) [9][10][11][12][13][14][15][16]59,60 demonstrates that all these radiocomplexes are effectively bound to bone tissue, mainly in the metabolically active bone compartments, and that they show long retention on bones. In conclusion, the shape and charge of the macrocyclic complex are not particularly important factors for the in vivo behavior of labeled macrocycle-bis(phosphonate) conjugates.…”

Section: Dalton Transactions Papermentioning

confidence: 99%

Cyclam with a phosphinate-bis(phosphonate) pendant arm is a bone-targeting carrier of copper radionuclides

et al. 2022

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“…Incubation of [ 68 Ga]Ga-PhenA-BPAMD in human plasma at 37 • C supported this assumption, showing progressively decreasing RCP over time (82.3%, 68.8%, and 46.7% at 30, 60, and 120 min, respectively). This significant drawback will have to be solved to confirm the relevance of incorporating AAZTA in bone-targeted theranostic agents, bearing in mind that some DOTA-containing analogues are already evaluated in humans for 68 Ga PET imaging [67] and 177 Lu therapy [68,69].…”

Section: Bisphosphonate Derivativesmentioning

confidence: 99%

AAZTA-Derived Chelators for the Design of Innovative Radiopharmaceuticals with Theranostic Applications

et al. 2022

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With the development of 68Ga and 177Lu radiochemistry, theranostic approaches in modern nuclear medicine enabling patient-centered personalized medicine applications have been growing in the last decade. In conjunction with the search for new relevant molecular targets, the design of innovative chelating agents to easily form stable complexes with various radiometals for theranostic applications has gained evident momentum. Initially conceived for magnetic resonance imaging applications, the chelating agent AAZTA features a mesocyclic seven-membered diazepane ring, conferring some of the properties of both acyclic and macrocyclic chelating agents. Described in the early 2000s, AAZTA and its derivatives exhibited interesting properties once complexed with metals and radiometals, combining a fast kinetic of formation with a slow kinetic of dissociation. Importantly, the extremely short coordination reaction times allowed by AAZTA derivatives were particularly suitable for short half-life radioelements (i.e., 68Ga). In view of these particular characteristics, the scope of this review is to provide a survey on the design, synthesis, and applications in the nuclear medicine/radiopharmacy field of AAZTA-derived chelators.

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Evaluation of Safety and Dosimetry of ¹⁷⁷Lu-DOTA-ZOL for Therapy of Bone Metastases

Cited by 24 publications

References 34 publications

Prognostic and Theranostic Applications of Positron Emission Tomography for a Personalized Approach to Metastatic Castration-Resistant Prostate Cancer

Prognostic and Theranostic Applications of Positron Emission Tomography for a Personalized Approach to Metastatic Castration-Resistant Prostate Cancer

Cyclam with a phosphinate-bis(phosphonate) pendant arm is a bone-targeting carrier of copper radionuclides

AAZTA-Derived Chelators for the Design of Innovative Radiopharmaceuticals with Theranostic Applications

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Evaluation of Safety and Dosimetry of 177Lu-DOTA-ZOL for Therapy of Bone Metastases

Cited by 24 publications

References 34 publications

Prognostic and Theranostic Applications of Positron Emission Tomography for a Personalized Approach to Metastatic Castration-Resistant Prostate Cancer

Prognostic and Theranostic Applications of Positron Emission Tomography for a Personalized Approach to Metastatic Castration-Resistant Prostate Cancer

Cyclam with a phosphinate-bis(phosphonate) pendant arm is a bone-targeting carrier of copper radionuclides

AAZTA-Derived Chelators for the Design of Innovative Radiopharmaceuticals with Theranostic Applications

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Product

Resources

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Evaluation of Safety and Dosimetry of ¹⁷⁷Lu-DOTA-ZOL for Therapy of Bone Metastases