Radiosynthesis involves the production of an analogue of the test substance in which one or more atoms have been replaced by a radioisotope. By radiolabeling a substance, it is possible to track its metabolism, decomposition and final fate in both animals and the environment. This tracking is essential to obtaining many safety assessment endpoints for plant production products (PPPs).
Most commonly, radiosynthesis involves the incorporation of a 14C label into the substance. The exact positioning of the 14C atom is critical so you can follow the fate of the molecule. In some instances, multiple radiolabelled substances are produced, with labels at different positions, so that the entire biotransformation of the substance is tracked.
- A dedicated team of chemists with extensive expertise in bespoke synthesis design, leading to high purity radiolabelled substances via chemical synthetic routes
- Proven track record for successful synthesis and purification of radiolabeled compounds
- Flexible facilities allow us to leverage capacity to meet your needs
Getting radiosynthesis right for your substance and endpoints
A high-purity radiolabeled test substance is vital for the success of a range of key safety assessment studies. But how best to label your substance? Can you use 14C or do you need an alternative? What labeling positions guarantee you can track all metabolites and degradation products? How pure is your radiolabeled test substance and can you properly identify it? How much substance do you need and how can you minimize expense? Have you got appropriate reference materials for the studies?
Excellence in radiosynthesis ensures downstream safety assessment success
Covance has a dedicated team of chemists with extensive expertise in the radiosynthesis and purification of test substances used in safety assessment of PPPs. Collaborative working between our radiochemists and metabolism scientists ensure that the radiosynthesis strategy reflects the needs driven by safety assessments endpoints. This optimizes the radiosynthesis of your test substance and ensures effective subsequent identification and characterization of the substance and its breakdown products.
In addition to in-house production of a synthesized test substance, we also have strong links with other commercial suppliers, and offer managed procurement of radiochemicals (where we cannot produce these in-house) and can assist in the sourcing of non-radiolabelled reference compounds or stable labeled analogues.
Experience with radiolabels and suppliers
Although 14C is a commonly used isotope in radiosynthesis, it is not appropriate for all substances. We have experience working with other isotopes such as 3H, 35S and 32P in radiosynthesis.
In addition to in-house production of a synthesized test substance, we also have strong links with other commercial suppliers, and offer managed procurement of radiochemicals (where we cannot produce these in-house) and can assist in the sourcing of non-radiolabeled reference compounds or stable labeled analogues.
Verified radiolabeled substances supported by detailed analytical data dossier
All synthesized products undergo analytical characterization for radiochemical purity and identify. The following checks are standard, resulting in a final certification of analysis:
- Radiochemical purity ≥97% (or as specified) confirmed using HPLC and/or TLC
- Chemical identity by co-chromatography with authentic reference compound
- Chemical identity by mass spectrometry
- Specific activity by mass spectrometry, HPLC-UV or gravimetric analysis
- Certificate of Analysis (QC and peer reviewed)
Facilities for radiosynthesis
We have four dedicated laboratories for radiosynthesis and purification equipped with a range of analytical tools:
- Liquid scintillation counters
- Flow through detection: radio and UV
- HPLC: analytical, semi-prep and preparative
- TLC detection: image analyzer
- LC-MS/MS analysis
- NMR analysis (with external partners)
- Access to Reaxys database search system for synthesis literature