Frank Scheffler will be attending the International Isotope Society workshop – 25th IIS-CED – from May 5th to 6th in Bad Soden, Germany.
Frank will present a poster on a client project in which a radiolabelled CYP derived metabolite was made using microbial biotransformation.
The International Isotope Society workshop on the synthesis and application of isotopes and isotopically labelled compounds.
Topics covered in the workshop:
- New methods in synthetic organic chemistry relevant to isotopic labelling
- Applications of radioactive and stable isotopically labelled compounds in research and biosciences
- PET chemistry
- New trends in analytics and measuring techniques
- Radioactive storage management and waste disposal
More information on Hypha’s capabilities in producing stable-labelled and radiolabelled metabolites.
Poster abstract – Microbial production of a radiolabelled metabolite of deflazacort for transporter substrate assay
We present a novel approach for preparing a radioactively labelled major human circulating metabolite of deflazacort for transporter substrate assays.
Delfazacort is a prodrug that is rapidly metabolised by esterases to the active metabolite 21-desacetyl deflazacort. Further metabolism by CYP3A4 results in hydroxylation to 6β-OH-21-desacetyl deflazacort, a major circulating plasma metabolite in humans.
Chemical synthesis routes to this metabolite are challenging due to multiple steps and the need for stereospecific reactions. Instead, microbial biotransformation was successfully used to make 14C-6β-OH-21-desacetyl deflazacort directly from the radiolabelled parent drug.
The poster will illustrate the steps undertaken to determine the best biotransformation process for making 14C-6β-OH-21-desacetyl deflazacort. This was done in two stages with the process first optimised to produce unlabelled 6β-OH-21-desacetyl deflazacort, identification of which was confirmed by NMR spectroscopy. The process was then repeated to make 14C-radiolabelled metabolite.