Bifunctional cyclam based ligands for conjugations with targeting vectors and their 64-Cu radiopharmaceuticals for PET imaging

Popis technologie

Název technologie: Bifunctional cyclam based ligands for conjugations with targeting vectors and their 64-Cu radiopharmaceuticals for PET imaging
Motivace: Wide range of radioisotopes is used in nuclear medicine for diagnostic and therapeutic applications. In the recent years, a number of metal radioisotopes have been considered as they enable nuclear medicine utilizations exactly according to patient needs. These radioisotopes cannot be applied in a free form as, in such form, they are non-specifically deposited in tissues. Therefore, the metal radioisotopes must be bound by suitable organic compounds (ligands) forming a stable complex.
Popis: Copper-64 is emerging PET radioisotope with half-life ~12 h and soft positron emission. Cyclam based ligands (= chelators), as highly selective chelators for copper over metallic impurities (e.g. nickel and zinc), were modified with a highly hydrophilic bis(phosphinate) pendant arm. Bifunctional chelators containing carboxylic, amine, isothiocyanate, azide or cyclooctyne groups were synthesized and conjugated to various substrates and biologically active targeting molecules (oligopeptides, antibodies or their fragments, folic acid, bis-phosphonates etc.). The chelators and their conjugates incorporate 64-Cu very efficiently even at room temperature and with very low chelator excess, producing radiopharmaceuticals with very high specific activities. The 64-Cu-labelled molecules are stable in-vivo with no non-specific deposition of the radiometal and easily excreted from body. The chelators represents a novel and unique family of ligands which has the best labelling efficiency among published copper chelators.
Komerční využití: The presented cyclam based ligands combined with copper radioisotopes can be used for visualization of biodistribution of many biologically active compounds using PET imaging. By leveraging this novel theranostic approach, our compounds allow the determination of dose during the diagnostic stage with Copper-64 and delivers the right amount of radiation to the tumor for therapy with Copper-67.
Status IP ochrany: International Patent Application published under PCT
Fáze vývoje technologie:

Fáze 2

Odpovídá TRL 3 a TRL 4

Výzkum proveditelnosti. Dochází k reálnému návrhu technologie a k prvotním testům v laboratoři vedoucím k upřesnění požadavků na technologii a jejích schopností.

  • TRL 3 představuje ucelenou představu na technologii s návrhem konkrétních kroků, testů a experimentů, které bude třeba uskutečnit, aby se ověřilo, že je nápad reálný
  • TRL 4 je ověření funkčnosti v laboratoři. Výsledkem TRL 4 představuje tzv. Proof-of-Concept. Technologie je tedy navržena a je ověřena její funkčnost v omezených podmínkách
Strategie pro hledání partnera: Licencování Spolupráce
Další informace: The group is able to prepare the bifunctional chelators up to a gram scale (if required) or to design/synthesize chelators tailored for a particular utilization.
Samples for radiolabelling tests are available on demand (MTA required).
Ilustrační obrázky: Žádný obrázek není vložen
Klíčová slova: diagnostics imaging radiopharmaceuticals screening
Kategorie: Farmacie Diagnostika
Vlastník technologie:
Instituce: Univerzita Karlova
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