68Ga-labeled DOTA-Peptides and 68Ga-labeled Radiopharmaceuticals for Positron Emission Tomography: Current Status of Research, Clinical Applications, and Future Perspectives

Breeman, W. A. P.; Blois, Erik de; Chan, Ho Sze; Konijnenberg, Mark; Kwekkeboom, Dik J.; Krenning, Eric P.

doi:10.1053/j.semnuclmed.2011.02.001

Cited by 180 publications

(109 citation statements)

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“…Neur oendocrine tumors can be diagnosed in vivo using PET with the radiolabeled somatostatin analogs 68 Ga-DOTATOC and 68 Ga-DOTATATE (1,2). Although the dosimetry of both tracers has been described separately (3,4) and has shown comparable effective doses, a comparative study using an identical, standardized methodology in a single group of patients has not been published and is of interest for tracer selection from a radiation dosimetry point of view.…”

mentioning

confidence: 99%

Comparative Biodistribution and Radiation Dosimetry of ⁶⁸Ga-DOTATOC and ⁶⁸Ga-DOTATATE in Patients with Neuroendocrine Tumors

et al. 2013

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68 Ga-DOTATOC and 68 Ga-DOTATATE are 2 radiolabeled somatostatin analogs for in vivo diagnosis of neuroendocrine tumors with PET. The aim of the present work was to measure their comparative biodistribution and radiation dosimetry. Methods: Ten patients diagnosed with neuroendocrine tumors were included. Each patient underwent a 45-min dynamic and 3 whole-body PET/CT scans at 1, 2, and 3 h after injection of each tracer on consecutive days. Absorbed doses were calculated using OLINDA/EXM 1.1. Results: Data from 9 patients could be included in the analysis. Of the major organs, the highest uptake at 1, 2, and 3 h after injection was observed in the spleen, followed by kidneys and liver. For both tracers, the highest absorbed organ doses were seen in the spleen and urinary bladder wall, followed by kidney, adrenals, and liver. The absorbed doses to the liver and gallbladder wall were slightly but significantly higher for 68 Ga-DOTATATE. The total effective dose was 0.021 6 0.003 mSv/MBq for both tracers. Conclusion: The effective dose for a typical 100-MBq administration of 68 Ga-DOTATATE and 68 Ga-DOTATOC is 2.1 mSv for both tracers. Therefore, from a radiation dosimetry point of view, there is no preference for either tracer for PET/CT evaluation of somatostatin receptor-expressing tumors.

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confidence: 99%

Comparative Biodistribution and Radiation Dosimetry of ⁶⁸Ga-DOTATOC and ⁶⁸Ga-DOTATATE in Patients with Neuroendocrine Tumors

et al. 2013

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“…Widespread application of the 68 Ge/ 68 Ga generator requires the development of protocols to make 68 Ga available for radiolabeling, because the eluate obtained is not necessarily suitable for direct medical use. First, the 68 Ga eluate contains measurable activities of the long-lived 68 Ge, which is a critical parameter in the context of the routine clinical application of 68 Ga-radiopharmaceuticals (1,2). Second, the relatively large volume and high acidity of the eluate hinder efficient radiolabeling and, thus, application in vivo.…”

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confidence: 99%

Ethanol-Based Post-processing of Generator-Derived ⁶⁸Ga Toward Kit-Type Preparation of ⁶⁸Ga-Radiopharmaceuticals

et al. 2014

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Post-processing by means of a cation-exchanger-based protocol is an efficient strategy for purification and concentration of generator-derived 68 Ga. It ensures the removal of 68 Ge before 68 Ga-radiopharmaceutical preparation and high labeling yields of 68 Ga-labeled radiopharmaceuticals for routine medical application. Methods: In an effort to overcome the problem associated with acetone in the currently applied method, we have investigated the feasibility of replacing it with ethanol. The purification of 68 Ga from coeluted metallic impurities ( 68 Ge 41 , Fe 31 , Zn 21 , and Ti 41 ) on various cation-exchange columns has been investigated with a variety of post-processing solutions. As a proof of principle, the post-processed 68 Ga was used to radiolabel DOTATOC in combination with high-purity water and various buffer solutions. Results: An effective protocol for the processing of generator-produced 68 Ga on the basis of cation-exchange chromatography using EtOH/HCl medium has been developed. Up to 95% of the initially eluted 68 Ga activity can be collected in a 1-mL fraction of 90% EtOH/0.9N HCl after removal of 68 Ge-breakthrough in a washing step. The post-processed eluate has been used to radiolabel DOTATOC in yields of approximately 97% ± 0.25% at 80°C in 5 min. Conclusion: The described novel protocol improves the radiolabeling efficiency and efficacy of DOTATOC, providing yields of greater than 99% (decay-corrected). As a result, further purification to separate the desired product from uncomplexed 68 Ga is not necessary. The developed post-processing and labeling protocols permit reliable and high-yield preparation of injectable 68 Ga-DOTATOC (or other 68 Ga-labeled radiopharmaceuticals) that are suitable for routine application. It is possible to incorporate this protocol into existing automated modules.

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“…Because of its matched half-life for tagging many biological processes and production method in a generator, 68 Ga is becoming an extremely important radioisotope in radiochemistry [46,47]. These generators contain a matrix with father isotope 68 Ge that present a long half-life of 270 days allowing the elution of 68 Ga for months, with the same generator.…”

Section: Nano-radiolabelling 221 Radioisotopesmentioning

confidence: 99%

Recent advances in the preparation and application of multifunctional iron oxide and liposome-based nanosystems for multimodal diagnosis and therapy

et al. 2016

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Nowadays, thanks to the successful discoveries in the biomedical field achieved in the last two decades, a deeper understanding about the complexity of mechanistic aspects of different pathological processes has been obtained. As a consequence, even the standard therapeutic protocols have undergone a vast redesign. In fact, the awareness about the necessity to progress towards a combined multitherapy in order to potentially increase the final healing chances has become a reality. One of the crucial elements of this novel approach is that large amounts of detailed information are highly needed and in vivo imaging techniques represent one of the most powerful tools to visualize and monitor the pathological state of the patient. To this scope, due to their unique features, nanostructured materials have emerged as attractive elements for the development of multifunctional tools for diagnosis and therapy. Hence, in this review, the most recent and relevant advances achieved by applying multifunctional nanostructures in multimodal theranosis of different diseases will be discussed. In more detail, the preparation and application of single multifunctional nano-radiotracers based on iron oxides and enabling PET/MRI dual imaging will be firstly detailed. After that, especially considering their highly promising clinical potential, the preparation and application of multifunctional liposomes useful for multimodal imaging and therapy will be reviewed. In both cases, a special focus will be set on the application of such a multifunctional nanocarriers in cancer as well as cardiovascular diseases.

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68Ga-labeled DOTA-Peptides and 68Ga-labeled Radiopharmaceuticals for Positron Emission Tomography: Current Status of Research, Clinical Applications, and Future Perspectives

Cited by 180 publications

References 70 publications

Comparative Biodistribution and Radiation Dosimetry of ⁶⁸Ga-DOTATOC and ⁶⁸Ga-DOTATATE in Patients with Neuroendocrine Tumors

Comparative Biodistribution and Radiation Dosimetry of ⁶⁸Ga-DOTATOC and ⁶⁸Ga-DOTATATE in Patients with Neuroendocrine Tumors

Ethanol-Based Post-processing of Generator-Derived ⁶⁸Ga Toward Kit-Type Preparation of ⁶⁸Ga-Radiopharmaceuticals

Recent advances in the preparation and application of multifunctional iron oxide and liposome-based nanosystems for multimodal diagnosis and therapy

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68Ga-labeled DOTA-Peptides and 68Ga-labeled Radiopharmaceuticals for Positron Emission Tomography: Current Status of Research, Clinical Applications, and Future Perspectives

Cited by 180 publications

References 70 publications

Comparative Biodistribution and Radiation Dosimetry of 68Ga-DOTATOC and 68Ga-DOTATATE in Patients with Neuroendocrine Tumors

Comparative Biodistribution and Radiation Dosimetry of 68Ga-DOTATOC and 68Ga-DOTATATE in Patients with Neuroendocrine Tumors

Ethanol-Based Post-processing of Generator-Derived 68Ga Toward Kit-Type Preparation of 68Ga-Radiopharmaceuticals

Recent advances in the preparation and application of multifunctional iron oxide and liposome-based nanosystems for multimodal diagnosis and therapy

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Resources

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Comparative Biodistribution and Radiation Dosimetry of ⁶⁸Ga-DOTATOC and ⁶⁸Ga-DOTATATE in Patients with Neuroendocrine Tumors

Comparative Biodistribution and Radiation Dosimetry of ⁶⁸Ga-DOTATOC and ⁶⁸Ga-DOTATATE in Patients with Neuroendocrine Tumors

Ethanol-Based Post-processing of Generator-Derived ⁶⁸Ga Toward Kit-Type Preparation of ⁶⁸Ga-Radiopharmaceuticals