The chemical tool-kit for molecular imaging with radionuclides in the age of targeted and immune therapy

Witney, Timothy H.; Blower, Philip J.

doi:10.1186/s40644-021-00385-8

Cited by 11 publications

(8 citation statements)

References 69 publications

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“…The nuclear medicine field relies on incorporating radioisotopes in small-molecule, nucleic acids, peptides, proteins, antibodies, and drug delivery technologies ( 1 – 3 ) that show high sensitivity for various diseases in order to impart diagnostic and therapeutic effects. Because of the same chemical properties, Copper-64 ( 64 Cu) and (Copper-67) 67 Cu can form chemical complexes using the identical labeling protocol, and diagnosis/therapy can be performed simultaneously ( 4 – 8 ).…”

Section: Introductionmentioning

confidence: 99%

Theragnostic 64Cu/67Cu Radioisotopes Production With RFT-30 Cyclotron

et al. 2022

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64Cu and 67Cu are theragnostic pair radionuclides with promising application in the nuclear medicine. 64Cu is PET nuclide for the non-invasive diagnosis and 67Cu is beta emitter for therapy of various cancers. This study discusses optimization efforts in the production of these radioactive coppers carried out with 30 MeV cyclotron. Optimized conditions include target preparation, chemical separation, and quality control. The production routes of 64Cu and 67Cu were studied based on the nuclear reactions of 64Ni(p,n)64Cu and 70Zn(p,α)67Cu. The produced 64Cu and 67Cu have >99.9% of the radionuclidic purity. The yield at the end of bombardment (EOB) of 64Cu and 67Cu is 28.5 MBq/μAh and 67Cu is 0.58 MBq/μAh, respectively.

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Section: Introductionmentioning

confidence: 99%

Theragnostic 64Cu/67Cu Radioisotopes Production With RFT-30 Cyclotron

et al. 2022

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“…Technetium-99m is a radioactive imaging transition metal supplied by Molybdenum -99/ Technetium -99 generators and considered as an expanded radioisotope having half-life time of 6 hours -140 KeV produced from Molybdenum-99 where Molybdenum -99 ( 99 Mo, (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20)Ci where 1Ci=37 GBq) that produced from highly or low enriched Uranium -235 reactors localized in Canada, Belgium, South Africa, France, Australia, and Argentina [4]. Production of Molybdenum-99(M0-99) routes are starting from U-235 or natural Mo-98 that targets with neutrons, U-238 or Mo-100 that targets with gamma, Zr-96 target with alpha ray and Mo-100 targets with proton [5].…”

Section: Table (1) Examples Of Various Radionuclides Isotopementioning

confidence: 99%

“…In contrast to Carbon -11, iodine-123, or Fluorine -18, Technetium -99m does not substituted any carbon or hydrogen atom in any pharmaceutical molecule to form Technetium -99m imaging agent or any labeling molecule [8].…”

Section: Table (1) Examples Of Various Radionuclides Isotopementioning

confidence: 99%

“…LD50 can be defined as the required dose of chemical that kills 50% (half) of the rats under test and ranges from toxic to nontoxic (safe) (in numbers, it ranges from less than 50 mg/Kg to more than 2000 mg/Kg). Table (3) and Figure (8) show medium lethal dose to rodent (LD50) ranged from (100-10000)mg/Kg calculated by https://tox-new.charite.de/protox_II/ while http://biosig.unimelb.edu.au/pkcsm/ showed Oral Rat Acute Toxicity (LD50) range (0.92 to 3.117) mol/Kg. LD50 values were influenced by PSA and logP and their determinants as mentioned above.…”

Section: Mag3-hbpmentioning

confidence: 99%

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Radioactive Imagine Agents: 99mTc-Toxicological Study

Hammud¹

2022

IJOIR

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Radioactive pharmaceutical materials (radiopharmaceuticals) that contain radioactive atom or/ and ion (emits nuclear (α, β, or / and γ) ray according to its energy and half-life duration) companied with organic or inorganic molecule are important materials in nuclear imaging or therapeutically medicine. Many biomolecules labeled with Technetium-99 in relationship to toxicity issues can be transported, distributed, and detected with the computerized algorithm detector depending upon chemical, biological, metabolic, and functional properties of tissue or organ (bone, liver, heart, kidney, and others). According to literatures' review about this subject, this is the first try in Iraq and other countries to study Technetium – radiomolecules with in Silico depending on two approachs. LD50, Class, Polar Surface Area PSA, logP, Hepatotoxicity, Carcinogenity, Immunotoxicity, Mutagenicity, Cytotoxicity, AMES test, Max. tolerated dose (human), hERG I and II inhibitor, Oral Rat Acute (LD50) and Chronic (LOAEL) Toxicity, Hepatotoxicity besides Skin Sensitisation showed that Tc-biomolecules under study are structurally unsafe having toxic response to liver, immune system, cellular components, DNA, and/or cardiac repolarization through hERG inhibition of action. These mainly conclusion notes depended upon Technetium oxidation state, heteroatoms presence, surface properties besides bio-target specifications, concentration, exposure time, genetic factors of human, and health problems.

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“…Radionuclides continue to be added to the toolbox of nuclear medicine, which represents an important field of development for drug discovery and nuclear medicine . Presently, fluorine-18( 18 F) and gallium-68( 68 Ga) are the most used positron emission tomography (PET) radionuclides for molecular imaging studies in nuclear medicine . PET permits noninvasive localization and quantification with relatively small amounts of radioactivity due to its high inherent sensitivity.…”

Section: Introductionmentioning

confidence: 99%

Zirconium Coordination Chemistry and Its Role in Optimizing Hydroxymate Chelation: Insights from Molecular Dynamics

Sormani,

Korde,

Rodriguez

et al. 2023

ACS Omega

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In the past decade, there has been a growth in using Zirconium-89 ( 89 Zr) as a radionuclide in nuclear medicine for cancer diagnostic imaging and drug discovery processes. Although one of the most popular chelators for 89 Zr, desferrioxamine (DFO) is typically presented as a hexadentate ligand, our work suggests a different scenario. The coordination structure of the Zr 4+ –DFO complex has primarily been informed by DFT-based calculations, which typically ignore temperature and therefore entropic and dynamic solvent effects. In this work, free energy calculations using molecular dynamics simulations, where the conformational fluctuations of both the ligand and the solvent are explicitly included, are used to compare the binding of Zr 4+ cations with two different chelators, DFO and 4HMS, the latter of which is an octadentate ligand that has been recently proposed as a better chelator due to the presence of four hydroxymate groups. We find that thermally induced disorder leads to an open hexadentate chelate structure of the Zr 4+ –DFO complex, leaving the Zr 4+ metal exposed to the solvent. A stable coordination of Zr 4+ with 4HMS, however, is formed by involving both hydroxamate groups and water molecules in a more closely packed structure.

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The chemical tool-kit for molecular imaging with radionuclides in the age of targeted and immune therapy

Cited by 11 publications

References 69 publications

Theragnostic 64Cu/67Cu Radioisotopes Production With RFT-30 Cyclotron

Theragnostic 64Cu/67Cu Radioisotopes Production With RFT-30 Cyclotron

Radioactive Imagine Agents: 99mTc-Toxicological Study

Zirconium Coordination Chemistry and Its Role in Optimizing Hydroxymate Chelation: Insights from Molecular Dynamics

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