Synthesis, characterization and biological evaluation of [188Re(N)(cys∼)(PNP)]+/0 mixed-ligand complexes as prototypes for the development of 188Re(N)-based target-specific radiopharmaceuticals

Thieme, Stefan Felix; Agostini, Stefania; Bergmann, Ralf; Pietzsch, Jens; Pietzsch, Hans‐Jürgen; Carta, Davide; Salvarese, Nicola; Refosco, Fiorenzo; Bolzati, Cristina

doi:10.1016/j.nucmedbio.2010.09.006

Cited by 12 publications

(12 citation statements)

References 33 publications

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“…Unfortunately, its very powerful donating nature is counterbalanced by its prominent chelating strength (NHˆS atom set). On the one hand, the latter ability contributes to stabilize the metal center [77, 80,81], on the other it becomes a disadvantage, in particular when an exchange reaction with another ligand has to be carried out to obtain the desired final complex in high yield and high specific activities [80,81].…”

Section: Preparation Of Nitrido Technetium-99m Radiopharmaceuticalsmentioning

confidence: 99%

“…Inorganics 2020, 8, 3 18 of 36 strength (NH^S atom set). On the one hand, the latter ability contributes to stabilize the metal center [77, 80,81], on the other it becomes a disadvantage, in particular when an exchange reaction with another ligand has to be carried out to obtain the desired final complex in high yield and high specific activities [80,81]. Thus, succinic dihydrazide (SDH) was selected owing to its water solubility, low toxicity, and lack of coordinating properties as a convenient source of N 3− atoms for the preparation of the [ 99m Tc][Tc≡N] core as a freeze-dry pharmaceutical kit.…”

Section: N 3− Donor [99mtc]tcn-rp % Rcy N 3− Donor [99mtc]tcn-rp % Rcymentioning

confidence: 99%

“…RGDEchi α v β 3 integrin/selective angiogenesis, tumor metastasis imaging [140] The pros and cons of the use of this technology have been summarized in a review by Bolzati et al [126] and compared with those of the other chemical approaches applied to the conjugation of targeting vectors. The procedure can be adapted to the 188 Re chemistry [80,81] and the compounds are well-defined from the chemical point of view. Again, the most important feature of this system is the heteroleptic nature of the final compounds, which affords a fine modulation of their physical and chemical properties: chelation systems can be carefully chosen (e.g., [S ∧ NH 2 ] − , [S ∧ O] 2− , and [S ∧ S] 2− ) to strike a suitable balance of the physical properties of the final compounds (charge, lipophilicity, etc.)…”

Section: Labeling Of Biologically Active Molecules: Target Specific Cmentioning

confidence: 99%

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Nitrido Technetium-99 m Core in Radiopharmaceutical Applications: Four Decades of Research

Bolzati

Dolmella

2019

Inorganics

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The knowledge on element 43 (Tc) of the periodic table, built over the years through the contributions given by the close relationship between chemistry and nuclear medicine, allowed the development of new and increasingly effective radiopharmaceuticals useful both as perfusion and target specific imaging agents for SPECT (single photon emission tomography). Among the manifold Tc-compounds, Tc(V) nitrido complexes played a relevant role in the search for new technetium-99m radiopharmaceuticals, providing efficient labeling procedures that can be conveniently exploited for the design and synthesis of agents, also incorporating small organic molecules or peptides having defined structural features. With this work, we present an overview of four decades of research on the chemistry and on the nuclear medicine applications of Tc(V) nitrido complexes.

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Section: Preparation Of Nitrido Technetium-99m Radiopharmaceuticalsmentioning

confidence: 99%

Section: N 3− Donor [99mtc]tcn-rp % Rcy N 3− Donor [99mtc]tcn-rp % Rcymentioning

confidence: 99%

Section: Labeling Of Biologically Active Molecules: Target Specific Cmentioning

confidence: 99%

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Nitrido Technetium-99 m Core in Radiopharmaceutical Applications: Four Decades of Research

Bolzati

Dolmella

2019

Inorganics

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“…If in the chemical structure of the incoming chelating ligand, a bioactive molecule is present, its selective interaction with the metal fragment would result in the formation of a stable final compound incorporating the bioactive substrate. On the basis of this strategy, different technetium and rhenium mixed-ligand compounds have been proposed for the development of target specific radiopharmaceuticals, among which the most representative examples are the [M(CO) 3 ] + [ 41 ] system, the [M(N)(PNP)] 2+ ( M = Tc, Re; PNP = phosphinoamine ligand) system [ 42 ], and the so-called “3+1” mixed-ligand system [ 43 ]. In particular, based on the “3+1” system, a new class of nitride 99m Tc and 188 Re theranostic agents was recently described [ 43 ].…”

Section: Design Of 188 Re Radiopharmaceuticalsmentioning

confidence: 99%

188Re(V) Nitrido Radiopharmaceuticals for Radionuclide Therapy

2017

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The favorable nuclear properties of rhenium-188 for therapeutic application are described, together with new methods for the preparation of high yield and stable 188Re radiopharmaceuticals characterized by the presence of the nitride rhenium core in their final chemical structure. 188Re is readily available from an 188W/188Re generator system and a parallelism between the general synthetic procedures applied for the preparation of nitride technetium-99m and rhenium-188 theranostics radiopharmaceuticals is reported. Although some differences between the chemical characteristics of the two metallic nitrido fragments are highlighted, it is apparent that the same general procedures developed for the labelling of biologically active molecules with technetium-99m can be applied to rhenium-188 with minor modification. The availability of these chemical strategies, that allow the obtainment, in very high yield and in physiological condition, of 188Re radiopharmaceuticals, gives a new attractive prospective to employ this radionuclide for therapeutic applications.

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“…Initial clinical trials showed that 188 Re-DEDC could be a useful radiopharmaceutical for unresectable HCC therapy. As another example, preparation and pre-clinical evaluation have also been reported for 188Re(N)(cys) (PNP), which is another example of a Re(V) nitrido complex, but clinical studies with this congener have evidently not yet been pursued[108].Finally, the combined synergistic application of188 Re-HEDP and other agents with chemotherapeutic agents may develop further. As an example, a recent Phase I safety study evaluated the combination of…”

mentioning

confidence: 99%

Important Clinical Applications of 188Rhenium for Radionuclide Therapy

Shinto¹

2017

Int. J. Nucl. Medi. Res.

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Although established clinical utility is of key importance in choosing agents for radionuclide therapy, other key factors include costs and GMP availability of sterile, pyrogen-free, regulatory approved radiopharmaceuticals. No-carrieradded (NCA) 188 Rhenium(188 Re, 16.9 hour half-life; 155 keV gamma emission) is available on demand as 188 Reperrhenate from saline elution of a 188 Tungsten/ 188 Rhenium(188 W/ 188 Re) generator. The availability and superb radionuclidic and chemical properties make 188 Re an excellent candidate for radionuclide therapy. This radioisotope is readily attached to a variety of targeting agents and also emits high energy beta particles (Emax 2.12 MeV) for therapy. Over the last 30 years the effectiveness of 188 Re for a variety of therapeutic applications has been established in multiple clinical studies. This overview provides a brief summary of clinical applications with 188 Re-labeled agents as an introduction to the detailed clinical discussions in the following papers. Although 188 Re-labeled radiopharmaceuticals for routine clinical use and accompanying reimbursement are not yet commercially available, several agents have been evaluated in clinical studies. In addition, a large number of 188 Re radiopharmaceutical agents have been developed and evaluated in pre-clinical studies over the last three decades. This review focuses on providing examples of 188 Re-labeled radiopharmaceutical agents which have entered late stage clinical use and have demonstrated good efficacy. These key applications include palliative treatment of skeletal metastases, intra-arterial therapy of liver cancer and post PTCA intravascular inhibition of arterial restenosis. Also, 188 Re radiopharmaceuticals had been developed and initially assessed for synovectomy and for marrow suppression. More recently, a unique device-based technology has entered clinical use for therapy of non-melanoma skin cancer using a 188 Re topical cream. Finally, 188 Re-antibodies are being developed for the potential therapy of infectious disease and this unique new therapeutic strategy is expected to enter clinical trials in the near future.

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Synthesis, characterization and biological evaluation of [188Re(N)(cys∼)(PNP)]+/0 mixed-ligand complexes as prototypes for the development of 188Re(N)-based target-specific radiopharmaceuticals

Cited by 12 publications

References 33 publications

Nitrido Technetium-99 m Core in Radiopharmaceutical Applications: Four Decades of Research

Nitrido Technetium-99 m Core in Radiopharmaceutical Applications: Four Decades of Research

188Re(V) Nitrido Radiopharmaceuticals for Radionuclide Therapy

Important Clinical Applications of 188Rhenium for Radionuclide Therapy

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