The chemistry of rhenium and technetium as related to the use of isotopes of these elements in therapeutic and diagnostic nuclear medicine

Deutsch, Edward; Libson, Karen; Vanderheyden, Jean-Luc; Ketring, Alan R.; Maxon, Harry R.

doi:10.1016/0883-2897(86)90027-9

Cited by 188 publications

(222 citation statements)

References 16 publications

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“…188 Re is a noteworthy therapeutic radionuclide with potential value in diagnosis because it emits both g rays (155 keV) and an extremely high energy of b particles (2.12 MeV) during decay. Its atomic radius is similar to technetium, and both radionuclides share common chemistry (9,10). Moreover, the tissue penetration of emitted b particles is only 5 mm, but it is sufficient to suppress the proliferation of human cancer cells with little damage to surrounding normal tissues (11).…”

mentioning

confidence: 99%

Evaluation of the Therapeutic and Diagnostic Effects of PEGylated Liposome–Embedded ¹⁸⁸Re on Human Non–Small Cell Lung Cancer Using an Orthotopic Small-Animal Model

Lin

Chang

et al. 2014

J Nucl Med

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Non-small cell lung cancer (NSCLC) is a highly morbid and mortal cancer type that is difficult to eradicate using conventional chemotherapy and radiotherapy. Little is known about whether radionuclide-based pharmaceuticals can be used for treating NSCLC. Here we embedded the therapeutic radionuclide 188 Re in PEGylated (PEG is polyethylene glycol) liposomes and investigated the biodistribution, pharmacokinetics, and therapeutic efficacy of this nanoradiopharmaceutical on NSCLC using a xenograft lung tumor model and the reporter gene imaging techniques. Methods: Human NSCLC NCI-H292 cells expressing multiple reporter genes were used in this study. 188 Re was conjugated to N,N-bis(2-mercaptoethyl)-N′,N′-diethylethylenediamine (BMEDA) and loaded into the PEGylated liposome to form a 188 Reliposome. The tumor growth rates and localizations were confirmed using bioluminescent imaging and SPECT/CT after the 188 Re-BMEDA or 188 Re-liposome was intravenously injected. The accumulation of the nanodrug in various organs was determined by the biodistribution analysis and the nano-SPECT/CT system. The pharmacokinetic and dosimetric analyses were further determined using WinNonlin and OLINDA/EXM, respectively. Results: The biodistribution and nano-SPECT/CT imaging showed that PEGylated 188 Re-liposome could efficiently accumulate in xenograft tumors formed by NCI-H292 cells that were subcutaneously implanted in nude mice. Pharmacokinetic analysis also showed that the retention of 188 Re-liposome was longer than that of 188 Re-BMEDA. In an orthotopic tumor model, ex vivo γ counting revealed that the uptake of 188 Re-liposome was detected in tumor lesions but not in surrounding normal lung tissues. Moreover, we evaluated the therapeutic efficacy using bioluminescent imaging and showed that the lung tumor growth was suppressed but not eradicated by 188 Re-liposome. The life span of 188 Re-liposometreated mice was 2-fold longer than that of untreated control mice. Conclusion:The results of biodistribution, pharmacokinetics, estimated dosimetry, nano-SPECT/CT, and bioluminescent imaging suggest that the PEGylated liposome-embedded 188 Re could be used for the treatment of human lung cancers.

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confidence: 99%

Evaluation of the Therapeutic and Diagnostic Effects of PEGylated Liposome–Embedded ¹⁸⁸Re on Human Non–Small Cell Lung Cancer Using an Orthotopic Small-Animal Model

Lin

Chang

et al. 2014

J Nucl Med

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“…In humans, the retention time in the heart is too short, probably due to a reduction of the complex to a neutral Tc(I1) species that washes out of the heart (5,6). Neutral ~~~~s -~~" T c ( D M P E ) , x~ was found to cross the blood-brain barrier in rats and thus might provide the basis for brain-perfusion imaging agents (7).…”

Section: Introductionmentioning

confidence: 99%

Molecular and crystal structure of a mixed-phosphine ligand Tc(II) complex, Tc(PMe₂Ph)₂(DMPE)Cl₂

Rochon¹,

Melanson²,

Kong³

1994

Can. J. Chem.

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The reaction of Tc(PMe,Ph),Cl, with an excess of bis(dimethy1phosphino)ethane (DMPE) in ethanol solution produced a yellow compound, which was identified by X-ray diffraction methods as a mixed-ligand Tc(I1) complex, TC(?M~,P~)~(DMPE)C~,.The compound crystallizes in the P2,lc space group with a = 12.899(6), b = 13.142(8), c = 19.088(9) A, P = 121.13(3)", V = 2770(2) A~, Z = 4, R = 0.061, and R,,, = 0.05 1. The geometry around the Tc atom is octahedral with the chloro ligands trnr~s to each other, while the two PMe,Ph ligands are in cis positions. The Tc-C1 bond distances are 2.43 l(5) and 2.43 l(5) A while the Tc-P bond lengths are 2.434(4) and 2.435(4) A for PMe,Ph and 2.400(4) and 2.398(4) A for the bidentate DMPE ligand. An increase of multiple bonding of the Tc-P bond, as the oxidation state of Tc decreases, is suggested. [Traduit par la rCdaction]

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“…Re and Tc complexes with the same ligand have essentially the same coordination parameters since the ionic radii of both metals are about the same due to the 'lanthanide contraction' effect. However, their chemistries do differ, for example, the higher oxidation states of Re are more stable and therefore reduced Re radiopharmaceuticals display a greater tendency to undergo re-oxidation to perrhenate [42].…”

Section: Rhenium Nitroimidazole Compoundsmentioning

confidence: 99%

Bifunctional Metal – Nitroimidazole Complexes for Hypoxia Theranosis in Cancer

Ricardo¹,

Kumar²,

Wiebe³

2015

J Diagn Imaging Ther

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Oxygen supply -demand imbalances can render proliferating cells acutely or chronically hypoxic. In cancer cells, hypoxia-induced pathophysiological changes give rise to genetic changes that lead to treatment-resistant, aggressive phenotypes. The reduced curability of hypoxic tumours by radiotherapy is one of consequent challenges, but their hypoxia also offers unique, exploitable properties. Nitroimidazoles, for example, capitalize on oxygen-sensitive reductive activation to achieve hypoxiaselective localization for theranostic consequence. The discovery of 2-nitroimidazole (azomycin) heralded the development of many drugs, including effective radiosensitizers of hypoxic cells. These electron-affinic, reductively bioactivated nitroheterocyclics undergo initial oxygen-reversible, enzymatic one-electron reductions that lead to the formation of molecular adducts that impair vital

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The chemistry of rhenium and technetium as related to the use of isotopes of these elements in therapeutic and diagnostic nuclear medicine

Cited by 188 publications

References 16 publications

Evaluation of the Therapeutic and Diagnostic Effects of PEGylated Liposome–Embedded ¹⁸⁸Re on Human Non–Small Cell Lung Cancer Using an Orthotopic Small-Animal Model

Evaluation of the Therapeutic and Diagnostic Effects of PEGylated Liposome–Embedded ¹⁸⁸Re on Human Non–Small Cell Lung Cancer Using an Orthotopic Small-Animal Model

Molecular and crystal structure of a mixed-phosphine ligand Tc(II) complex, Tc(PMe₂Ph)₂(DMPE)Cl₂

Bifunctional Metal – Nitroimidazole Complexes for Hypoxia Theranosis in Cancer

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The chemistry of rhenium and technetium as related to the use of isotopes of these elements in therapeutic and diagnostic nuclear medicine

Cited by 188 publications

References 16 publications

Evaluation of the Therapeutic and Diagnostic Effects of PEGylated Liposome–Embedded 188Re on Human Non–Small Cell Lung Cancer Using an Orthotopic Small-Animal Model

Evaluation of the Therapeutic and Diagnostic Effects of PEGylated Liposome–Embedded 188Re on Human Non–Small Cell Lung Cancer Using an Orthotopic Small-Animal Model

Molecular and crystal structure of a mixed-phosphine ligand Tc(II) complex, Tc(PMe2Ph)2(DMPE)Cl2

Bifunctional Metal – Nitroimidazole Complexes for Hypoxia Theranosis in Cancer

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Evaluation of the Therapeutic and Diagnostic Effects of PEGylated Liposome–Embedded ¹⁸⁸Re on Human Non–Small Cell Lung Cancer Using an Orthotopic Small-Animal Model

Evaluation of the Therapeutic and Diagnostic Effects of PEGylated Liposome–Embedded ¹⁸⁸Re on Human Non–Small Cell Lung Cancer Using an Orthotopic Small-Animal Model

Molecular and crystal structure of a mixed-phosphine ligand Tc(II) complex, Tc(PMe₂Ph)₂(DMPE)Cl₂