ReviewMolecules (Basel, Switzerland)2015
Methods to Increase the Metabolic Stability of (18)F-Radiotracers.
Review in Molecules (Basel, Switzerland), 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.
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Who cites it
44 citing papers in PubMed, 88 citations in OpenAlex.
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- Stability assessment of PET radiopharmaceuticals under extreme conditions: an ICH-compliant study on radiochemical and enantiomeric purity.EJNMMI radiopharmacy and chemistry · 2025Article
- Structure-Property Relationships Reported for the New Drugs Approved in 2024.Mini reviews in medicinal chemistry · 2025Review
- The [18F] F-PSMA Probe: Chemical Perspectives.Current medicinal chemistry · 2025Review
- Development and evaluation of deuterated [EJNMMI radiopharmacy and chemistry · 2024Article
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- Metabolic Stability of the Demyelination Positron Emission Tomography Tracer [The Journal of pharmacology and experimental therapeutics · 2023Article
- Radiochemistry for positron emission tomography.Nature communications · 2023Review
- Automated Synthesis of [Pharmaceuticals (Basel, Switzerland) · 2023Article
- Investigation of Radiotracer Metabolic Stability In Vitro with CYP-Overexpressing Hepatoma Cell Lines.Cells · 2022Article
- [Nature · 2022Article
- Arene radiofluorination enabled by photoredox-mediated halide interconversion.Nature chemistry · 2022Article
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The majority of pharmaceuticals and other organic compounds incorporating radiotracers that are considered foreign to the body undergo metabolic changes in vivo. Metabolic degradation of these drugs is commonly caused by a system of enzymes of low substrate specificity requirement, which is present mainly in the liver, but drug metabolism may also take place in the kidneys or other organs. Thus, radiotracers and all other pharmaceuticals are faced with enormous challenges to maintain their stability in vivo highlighting the importance of their structure. Often in practice, such biologically active molecules exhibit these properties in vitro, but fail during in vivo studies due to obtaining an increased metabolism within minutes. Many pharmacologically and biologically interesting compounds never see application due to their lack of stability. One of the most important issues of radiotracers development based on fluorine-18 is the stability in vitro and in vivo. Sometimes, the metabolism of (18)F-radiotracers goes along with the cleavage of the C-F bond and with the rejection of [(18)F]fluoride mostly combined with high background and accumulation in the skeleton. This review deals with the impact of radiodefluorination and with approaches to stabilize the C-F bond to avoid the cleavage between fluorine and carbon.
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