ArticleJournal of the American Chemical Society2013
H(4)octapa-trastuzumab: versatile acyclic chelate system for 111In and 177Lu imaging and therapy.
Article in Journal of the American Chemical Society, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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Who cites it
28 citing papers in PubMed, 89 citations in OpenAlex.
- Article
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- Chemical Tools to Characterize the Coordination Chemistry of Radionuclides for Radiopharmaceutical Applications.Chemical reviews · 2025Review
- Decadentate Acyclic Chelators for Lanthanum Radiopharmaceuticals.Journal of medicinal chemistry · 2025Article
- Targeted radiopharmaceuticals: an underexplored strategy for ovarian cancer.Theranostics · 2024Review
- Radiometallation and photo-triggered release of ready-to-inject radiopharmaceuticals from the solid phase.Chemical science · 2023Article
- Glypican-3-TargetedJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2022Article
- Development of a multi faceted platform containing a tetrazine, fluorophore and chelator: synthesis, characterization, radiolabeling, and immuno-SPECT imaging.EJNMMI radiopharmacy and chemistry · 2022Article
- The Chemical Scaffold of Theranostic Radiopharmaceuticals: Radionuclide, Bifunctional Chelator, and Pharmacokinetics Modifying Linker.Molecules (Basel, Switzerland) · 2022Review
- Versatile Macrocyclic Platform for the Complexation of [Inorganic chemistry · 2022Article
- Rigidified Derivative of the Non-macrocyclic Ligand HInorganic chemistry · 2022Article
- Stable Chelation of the Uranyl Ion by Acyclic Hexadentate Ligands: Potential Applications forInorganic chemistry · 2022Article
- AAZTA-Derived Chelators for the Design of Innovative Radiopharmaceuticals with Theranostic Applications.Pharmaceuticals (Basel, Switzerland) · 2022Review
- A Systematic Evaluation of Antibody Modification andBioconjugate chemistry · 2021Article
- PET imaging facilitates antibody screening for synergistic radioimmunotherapy with aTheranostics · 2021Article
- Oxyaapa: A Picolinate-Based Ligand with Five Oxygen Donors that Strongly Chelates Lanthanides.Inorganic chemistry · 2020Article
- Radiolabelled Peptides for Positron Emission Tomography and Endoradiotherapy in Oncology.Pharmaceuticals (Basel, Switzerland) · 2020Review
- Evaluation of polydentate picolinic acid chelating ligands and an α-melanocyte-stimulating hormone derivative for targeted alpha therapy using ISOL-producedEJNMMI radiopharmacy and chemistry · 2019Article
- Preclinical evaluation ofOncology letters · 2018Article
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 2 countries.
Funding
Abstract
A bifunctional derivative of the versatile acyclic chelator H4octapa, p-SCN-Bn-H4octapa, has been synthesized for the first time. The chelator was conjugated to the HER2/neu-targeting antibody trastuzumab and labeled in high radiochemical purity and specific activity with the radioisotopes (111)In and (177)Lu. The in vivo behavior of the resulting radioimmunoconjugates was investigated in mice bearing ovarian cancer xenografts and compared to analogous radioimmunoconjugates employing the ubiquitous chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA). The H4octapa-trastuzumab conjugates displayed faster radiolabeling kinetics with more reproducible yields under milder conditions (15 min, RT, ~94-95%) than those based on DOTA-trastuzumab (60 min, 37 °C, ~50-88%). Further, antibody integrity was better preserved in the (111)In- and (177)Lu-octapa-trastuzumab constructs, with immunoreactive fractions of 0.99 for each compared to 0.93-0.95 for (111)In- and (177)Lu-DOTA-trastuzumab. These results translated to improved in vivo biodistribution profiles and SPECT imaging results for (111)In- and (177)Lu-octapa-trastuzumab compared to (111)In- and (177)Lu-DOTA-trastuzumab, with increased tumor uptake and higher tumor-to-tissue activity ratios.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.