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Nuclear Medicine and Biology

2007

DOI: 10.1016/j.nucmedbio.2007.06.016

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A comparative study of 188Re(V)-meso-DMSA and 188Re(V)-rac-DMSA: preparation and in vivo evaluation in nude mice xenografted with a neuroendocrine tumor

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Cited by 9 publications

(3 citation statements)

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“…The DMSA ligand exists as two isomers, racemic and meso, and the biological properties of the 188 Re (and 99m Tc) complexes of the two isomers are somewhat different. Although initial human studies were carried out with the meso isomer, more recent preclinical studies suggest that the tumor uptake of the 188 Re complexes of the rac isomer is higher with lower uptake in normal bone . These investigators also found that the synthesis conditions required to obtain optimal yield were somewhat different for the two isomers with a higher concentration of sodium metabisulfite and ligand and a higher pH required to prepare the Re(V) complex of the rac isomer.…”

Section: Rheniummentioning

confidence: 99%

Radioactive Transition Metals for Imaging and Therapy

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2018

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Nuclear medicine is composed of two complementary areas, imaging and therapy. Positron emission tomography (PET) and single-photon imaging, including single-photon emission computed tomography (SPECT), comprise the imaging component of nuclear medicine. These areas are distinct in that they exploit different nuclear decay processes and also different imaging technologies. In PET, images are created from the 511 keV photons produced when the positron emitted by a radionuclide encounters an electron and is annihilated. In contrast, in single-photon imaging, images are created from the γ rays (and occasionally X-rays) directly emitted by the nucleus. Therapeutic nuclear medicine uses particulate radiation such as Auger or conversion electrons or β − or α particles. All three of these technologies are linked by the requirement that the radionuclide must be attached to a suitable vector that can deliver it to its target. It is imperative that the radionuclide remain attached to the vector before it is delivered to its target as well as after it reaches its target or else the resulting image (or therapeutic outcome) will not reflect the biological process of interest. Radiochemistry is at the core of this process, and radiometals offer radiopharmaceutical chemists a tremendous range of options with which to accomplish these goals. They also offer a wide range of options in terms of radionuclide half-lives and emission properties, providing the ability to carefully match the decay properties with the desired outcome. This Review provides an overview of some of the ways this can be accomplished as well as several historical examples of some of the limitations of earlier metalloradiopharmaceuticals and the ways that new technologies, primarily related to radionuclide production, have provided solutions to these problems.

“…The DMSA ligand exists as two isomers, racemic and meso, and the biological properties of the 188 Re (and 99m Tc) complexes of the two isomers are somewhat different. Although initial human studies were carried out with the meso isomer, more recent preclinical studies suggest that the tumor uptake of the 188 Re complexes of the rac isomer is higher with lower uptake in normal bone . These investigators also found that the synthesis conditions required to obtain optimal yield were somewhat different for the two isomers with a higher concentration of sodium metabisulfite and ligand and a higher pH required to prepare the Re(V) complex of the rac isomer.…”

Section: Rheniummentioning

confidence: 99%

Radioactive Transition Metals for Imaging and Therapy

¹

,

²

2018

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Nuclear medicine is composed of two complementary areas, imaging and therapy. Positron emission tomography (PET) and single-photon imaging, including single-photon emission computed tomography (SPECT), comprise the imaging component of nuclear medicine. These areas are distinct in that they exploit different nuclear decay processes and also different imaging technologies. In PET, images are created from the 511 keV photons produced when the positron emitted by a radionuclide encounters an electron and is annihilated. In contrast, in single-photon imaging, images are created from the γ rays (and occasionally X-rays) directly emitted by the nucleus. Therapeutic nuclear medicine uses particulate radiation such as Auger or conversion electrons or β − or α particles. All three of these technologies are linked by the requirement that the radionuclide must be attached to a suitable vector that can deliver it to its target. It is imperative that the radionuclide remain attached to the vector before it is delivered to its target as well as after it reaches its target or else the resulting image (or therapeutic outcome) will not reflect the biological process of interest. Radiochemistry is at the core of this process, and radiometals offer radiopharmaceutical chemists a tremendous range of options with which to accomplish these goals. They also offer a wide range of options in terms of radionuclide half-lives and emission properties, providing the ability to carefully match the decay properties with the desired outcome. This Review provides an overview of some of the ways this can be accomplished as well as several historical examples of some of the limitations of earlier metalloradiopharmaceuticals and the ways that new technologies, primarily related to radionuclide production, have provided solutions to these problems.

“…In addition, we chose [21,29,30]. Park et al [30] postulated the high uptake of 188 Re-compound in the stomach to be related to the acidic environment in the stomach of mice rather than an outcome of catabolism. In our study, we obtained satisfactory results of in vitro stability.…”

Section: Discussionmentioning

confidence: 99%

A study on the preparation, evaluation of biological characteristics, and preliminary imaging of [188Re]Re-ibandronate

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Background Bone is a common site of metastasis of malignant tumor. Several radiopharmaceuticals are available to relieve bone pain in patients with cancer. However, there is still a need to to investigate easily accessible and high bone affinity radiopharmaceuticals. Radionuclide 188Re has an advantage in this regard because of its commercial extraction from 188W/188Re generators. It can be used on demand and is cost-effective. The first-generation bisphosphonate hydroxyethylidene diphosphonate (HEDP) is the commonly used bisphosphonate for 188Re-labelling. And the third-generation bisphosphonates ibandronate (IBA) has higher bone affinity and ability to inhibit bone resorption than HEDP. However, there have been no reports on 188Re-labelling with IBA. We used IBA and 188Re for radiolabeling to develop and evaluate a novel type of bone-seeking radiopharmaceutical. Results We successfully prepared [188Re]Re-IBA in > 95% RCP. The optimum preparation conditions were as follows: IBA, 1.2–1.6 mg; ascorbic acid, 0.20–0.35 mg; stannous chloride, 0.14–0.18 mg; potassium perrhenate, 0.005–0.009 mg; and [188Re]ReO4− activity, 18.5–55 MBq, were reacted for 30 min at 95℃ and pH = 2. [188Re]Re-IBA demonstrated good stability in vitro, high plasma protein binding rate, and good hydrophilicity. The in vivo distribution of mice and bone imaging in New Zealand rabbits showed high bone uptake, long retention time, rapid blood clearance, and relatively low soft tissue uptake. Conclusion Our study encompassed the successful preparation of [188Re]Re-IBA, a novel bone-seeking radiopharmaceutical, and confirmed it has great potential for the treatment of bone pain and imaging monitoring.

“…Further study showed that the individual isomers showed no significant differences in biodistribution, and underwent interconversion, in rats [42] and (in the case of [ 99m TcO(DMSA) 2 ] -) in humans [43]. The analogous complexes of the racemic DMSA ligand (Figure 3c) were evaluated [44] in PC-12 tumours in nude mice and showed higher tumour uptake than the meso- complexes. A range of ester derivatives of the complexes showed promising tumour uptake and reduced bone uptake in animal models [45].…”

Section: Rhenium (V) Complexesmentioning

confidence: 99%

Rhenium-188 Radiochemistry: Challenges and Prospects

2017

Int. J. Nucl. Medi. Res.

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After a lull in development of new chemistry for rhenium-188 and technetium-99m since 2000, there has been new investment in production facilities for Mo-99/Tc-99m coupled with increasing interest in rhenium-188 radionuclide therapy, particularly in developing countries. Much of the chemistry developed in the 1990s is not readily amenable to supporting modern radiopharmaceutical development, which places increased emphasis on molecular targeted radiopharmaceuticals. Consequently there is a need for new radiolabelling chemistry to incorporate these radionuclides into biomolecules using simple, kit-based methodology. This review provides an update on progress towards simple rhenium-188 labelling methods since 2000.

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