Bifunctional chelators for radiorhenium: past, present and future outlook.
Diana R MelisAndrew R BurgoyneMaarten OomsGilles GasserPublished in: RSC medicinal chemistry (2022)
Targeted radionuclide therapy (TRNT) is an ever-expanding field of nuclear medicine that provides a personalised approach to cancer treatment while limiting toxicity to normal tissues. It involves the radiolabelling of a biological targeting vector with an appropriate therapeutic radionuclide, often facilitated by the use of a bifunctional chelator (BFC) to stably link the two entities. The radioisotopes of rhenium, 186 Re ( t 1/2 = 90 h, 1.07 MeV β - , 137 keV γ (9%)) and 188 Re ( t 1/2 = 16.9 h, 2.12 MeV β - , 155 keV γ (15%)), are particularly attractive for radiotherapy because of their convenient and high-abundance β - -particle emissions as well as their imageable γ-emissions and chemical similarity to technetium. As a transition metal element with multiple oxidation states and coordination numbers accessible for complexation, there is great opportunity available when it comes to developing novel BFCs for rhenium. The purpose of this review is to provide a recap on some of the past successes and failings, as well as show some more current efforts in the design of BFCs for 186/188 Re. Future use of these radionuclides for radiotherapy depends on their cost-effective availability and this will also be discussed. Finally, bioconjugation strategies for radiolabelling biomolecules with 186/188 Re will be touched upon.
Keyphrases
- transition metal
- early stage
- locally advanced
- cancer therapy
- radiation induced
- radiation therapy
- municipal solid waste
- dual energy
- highly efficient
- gene expression
- life cycle
- oxidative stress
- metal organic framework
- rectal cancer
- current status
- squamous cell carcinoma
- hydrogen peroxide
- computed tomography
- antibiotic resistance genes
- mesenchymal stem cells
- nitric oxide
- wastewater treatment