A5016804317- Radiopharmaceutical Chemistry and Applications
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Medical Imaging Techniques and Applications
- Medical Imaging and Pathology Studies
- Radioactive element chemistry and processing
- Lanthanide and Transition Metal Complexes
- Boron Compounds in Chemistry
- Chemical Synthesis and Characterization
- Nuclear Physics and Applications
- Radioactive Decay and Measurement Techniques
- Chemical Reactions and Isotopes
- Radiation Therapy and Dosimetry
- Metal complexes synthesis and properties
- Peptidase Inhibition and Analysis
- Inorganic Fluorides and Related Compounds
- Lung Cancer Treatments and Mutations
- Magnetism in coordination complexes
- Chemical Synthesis and Analysis
- Metal-Catalyzed Oxygenation Mechanisms
- Monoclonal and Polyclonal Antibodies Research
- HER2/EGFR in Cancer Research
- Inorganic and Organometallic Chemistry
- Click Chemistry and Applications
- Thallium and Germanium Studies
TRIUMF
2016-2025
Simon Fraser University
2011-2025
Robert Bosch (Germany)
2024
University of British Columbia
2013-2016
Vancouver Biotech (Canada)
2016
Health Canada
2010
Abstract The 18‐membered macrocycle H 2 macropa was investigated for 225 Ac chelation in targeted alpha therapy (TAT). Radiolabeling studies showed that macropa, at submicromolar concentration, complexed all (26 kBq) 5 min RT. [ Ac(macropa)] + remained intact over 7 to 8 days when challenged with either excess La 3+ ions or human serum, and did not accumulate any organ after h healthy mice. A bifunctional analogue, macropa‐NCS, conjugated trastuzumab as well the prostate‐specific membrane...
Abstract Background Lead-212 ( 212 Pb, t 1/2 = 10.6 h) and lead-203 203 51.9 are an element-equivalent, or a matched theranostic radioisotope pair that show great potential for application in targeted radionuclide therapy (TRT) single-photon emission computed tomography (SPECT), respectively. At TRIUMF we have produced both Pb using TRIUMF’s TR13 (13 MeV) 500 MeV cyclotrons, subsequently purified evaluated radioisotopes series of pyridine-modified DOTA analogues comparison to the...
The neutral and one-electron oxidized group 10 metal, Ni(II), Pd(II) Pt(II), six-membered chelate Salpn (Salpn = N,N'-bis(3,5-di-tert-butylsalicylidene)-1,3-propanediamine) complexes have been investigated compared to the five-membered Salen (N,N'-bis(3,5-di-tert-butylsalicylidene)-1,2-ethanediamine) Salcn (N,N'-bis(3,5-di-tert-butylsalicylidene)-1,2-cyclohexane-(1R,2R)-diamine) complexes. Reaction of with 1 equivalent AgSbF(6) affords which exist as ligand radical species in solution solid...
A bifunctional derivative of the versatile acyclic chelator H4octapa, p-SCN-Bn-H4octapa, has been synthesized for first time. The was conjugated to HER2/neu-targeting antibody trastuzumab and labeled in high radiochemical purity specific activity with radioisotopes (111)In (177)Lu. vivo behavior resulting radioimmunoconjugates investigated mice bearing ovarian cancer xenografts compared analogous employing ubiquitous 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)....
The synthesis of the octadentate bispidine ligand bearing two picolinic acid pendant arms (H2 bispa2 ), and its coordination chemistry with radionuclides relevant for nuclear medicine, namely indium(III) (111 In), lutetium(III) (177 Lu), lanthanum(III) (as surrogate 225 Ac), are reported. non-radioactive metal complexes N6 O2 -type bispa were characterized by 1 H 13 C NMR spectroscopy, elemental analysis, mass spectrometry single-crystal X-ray analysis. Experimental structural data,...
Nuclear medicine leverages different types of radiometals for disease diagnosis and treatment, but these applications usually require them to be stably chelated. Given the often-disparate chemical properties radionuclides, it is challenging find a single chelator that binds all effectively. Toward addressing this problem, we recently reported macrocyclic macrodipa with an unprecedented "dual-size-selectivity" pattern lanthanide (Ln3+) ions, characterized by its high affinity both large small...
The chiral acyclic ligands H2CHXdedpa (N4O2), H2CHXdedpa-bb and H4CHXoctapa (N4O4) (CHX = cyclohexyl/cyclohexane, H2dedpa 1,2-[[6-carboxy-pyridin-2-yl]-methylamino]ethane, bb N,N′-dibenzylated, H4octapa N,N′-bis(6-carboxy-2-pyridylmethyl)-ethylenediamine-N,N′-diacetic acid) were synthesized, complexed with Ga(III) and/or In(III), evaluated for their potential as chelating agents in radiopharmaceutical applications. compared to the previously studied hexadentate octadentate determine effect...
Effective use of the decay chain in targeted internal radioimmunotherapy requires retention both and progeny isotopes at target site. Imaging-based pharmacokinetic tests these pharmaceuticals must therefore separately yet simultaneously image multiple that may not be colocalized despite being part same chain. This work presents feasibility studies demonstrating ability a microSPECT/CT scanner equipped with high energy collimator to two components chain: (218 keV) (440 keV). Image quality...
Actinium-225 (225Ac, t1/2 = 9.9 d) is a promising candidate radionuclide for use in targeted alpha therapy (TAT), though the currently limited global supply has hindered development of suitable Ac-chelating ligand and 225Ac-radiopharmaceuticals towards clinic. We at TRIUMF have leveraged our Isotope Separation On-Line (ISOL) facility to produce 225Ac resulting radioactivity screen number potential 225Ac-radiopharmaceutical compounds.MBq quantities parent radium-225 (225Ra, 14.8 were produced...
The radionuclide 213Bi can be applied for targeted α therapy (TAT): a type of nuclear medicine that harnesses particles to eradicate cancer cells. To use this application, bifunctional chelator (BFC) is needed attach it biological targeting vector deliver selectively Here, we investigated six macrocyclic ligands as potential BFCs, fully characterizing the Bi3+ complexes by NMR spectroscopy, mass spectrometry, and elemental analysis. Solid-state structures three revealed distorted...
TRIUMF is one of the only laboratories in world able to produce both lead-203 (203Pb, t1/2 = 51.9 h) and 212Pb (t1/2 10.6 onsite via its 13 500 MeV cyclotrons, respectively. Together, 203Pb form an element-equivalent theranostic pair that potentiate image-guided, personalized cancer treatment, using as a single-photon emission computed tomography (SPECT) source, for targeted alpha therapy. In this study, improvements production were accomplished by manufacturing electroplated, silver-backed...
A series of macrocyclic ligands were considered for the chelation Pb2+: 1,4,7,10-tetrakis[2-(methylsulfanyl)ethyl]-1,4,7,10-tetraazacyclododecane (DO4S), 1,4,7-tris[2-(methylsulfanyl)ethyl]-1,4,7,10-tetraazacyclododecane (DO3S), 1,4,7-tris[2-(methylsulfanyl)ethyl]-10-acetamido-1,4,7,10-tetraazacyclododecane (DO3SAm), 1,7-bis[2-(methylsulfanyl)ethyl]-1,4,7,10-tetraazacyclododecane-4,10-diacetic acid (DO2A2S), 1,5,9-tris[2-(methylsulfanyl)ethyl]-1,5,9-triazacyclododecane (TACD3S),...
The development of inert, biocompatible chelation methods is required to harness the emerging positron emitting radionuclide
TRIUMF has a long history of medical isotope production. For more than 40 years, the Life Sciences Division at produced isotopes for Positron Emission Tomography (PET) local hospitals. Recently, division taken on challenge to expand facility's repertoire imaging treatment. At smallest cyclotron with energy 13 MeV, radiometals are being in liquid target which is typically used PET This effort makes available early stage research and preclinical trials. beam 24 we produce 99mTc from 100Mo...
Correction for ‘Exploring the use of rigid 18-membered macrocycles with amide pendant arms Pb( ii )-based radiopharmaceuticals’ by Charlene Harriswangler et al. , Inorg. Chem. Front. 2024, 11 1070–1086, https://doi.org/10.1039/D3QI02354K.
<title>Abstract</title> <bold>Background</bold> Antimony-119 (<sup>119</sup>Sb, t<sub>1/2 </sub>= 38.19 h) is an Auger electron emitting radionuclide of interest for radiopharmaceutical therapy. It can be directly produced by proton bombardment tin-119 using low energy cyclotrons. The radiochemical separation methods available recovering <sup>119</sup>Sb from the bulk Sn target material are lacking, particularly with respect to matrix suitability further applications. <bold>Results</bold>...
The geometric and electronic structure of a bimetallic Ni Schiff-base complex its one-electron oxidized form have been investigated in the solid state solution. two salen units neutral 1 are linked via bridging catecholate function. [1](+) was determined to exist as ligand radical species solution, with electron hole potentially localized on redox-active dioxolene, phenolate ligands, or delocalized over entire system. Electrochemical experiments UV-vis-NIR spectroscopy, combination density...
Potentially nonadentate (N5O4) bifunctional chelator p-SCN-Bn-H4neunpa and its immunoconjugate H4neunpa-trastuzumab for 111In radiolabeling are synthesized. The ability of to quantitatively radiolabel 111InCl3 at an ambient temperature within 15 or 30 min, respectively, is presented. Thermodynamic stability determination with In3+, Bi3+, La3+ resulted in high conditional constant (pM) values. In vitro human serum assays have demonstrated both complexes over 5 days. Mouse biodistribution...