Biotransformation
Phase I & Phase II metabolites of xenobiotics need to be identified and caracterize as they may have new or modified activities and/or improved bioavailability compared to their parent compound. Furthermore, according to Safety testing of drug metabolite guidance for industry from the FDA, and under certain circunstances assessment of metabolite safety is required. However, these derivates may be difficult to produce using classic chemical synthesis.
Therefore, Bertin Pharma offers a fully integrated analytical and preparative platform using biotransformation and/or chemoenzymatic technologies for the production of Phase I metabolites and Conjugated metabolites (mainly glucuronide or sulfate derivatives). This platform gathers:
A collection of- 200 non pathogenic bacterial strains, filamentous fungi or yeasts able to
mimic most of the chemical reactions performed by mammalian cytochomes P450)
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Genetically modified yeast over-expressing human CYP 450
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Selected microbial strains able to directly generate conjugation reactions classically
found in mammalian drug metabolism
(glucosylation, glucuronidation, sulfatation)
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Various animal microsomal fractions containing the relevant UGTs (Uridine
diphosphoglucuronyl transferases) in specific
preparative conditions
A screening method based on a 96 well plate technology to select the best microorganisms to perform the desired biotransformation upon synthetic or natural compounds of interest.
Production facilities to biosynthesise metabolites from few milligrams to several grams including downstream process (extraction and purification facilities)
State-of-the art analytical facilities to identify and quantify drugs using LC/MS, LC/MS/MS, EIA, RIA.
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Applications & technological advantages
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Overproduction of minor metabolites
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Production of internal standards and “authentic” metabolic controls available for human and animal studies
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Panel of complementary technologies from chemical to biochemical methods to select the more efficient pathway, depending on the targeted preparative scale
Selective microbiological transformation allowing regio- and/or stereospecificity
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Possible regioselectivity of glucuronidation reaction on polyhydroxylated metabolites
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Production scale<
: from few milligrams to grams
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Lower cost of
the biological methods, at the laboratory level, compared to the chemical synthesis, as far as complex and sensitive molecules are concerned involving numerous protection and deprotection steps
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Enables to get access to molecules difficult to gain by classic chemistry approach
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Biotransformation equipment platform - Spectrophotometer
- Spectrofluorimeter
- HPLC/UV systems
- Microorganisms collection
Your advantages for working with us
- shorten process time
- reduce cost
- alternative to complex chemical synthesis
- production scale (from few milligrams to grams)
- possible regioselectivity of glucuronidation reaction on polyhydroxylated metabolites
If you wish more details about our Biotransformation services, feel free to contact us.
______________________________________________________________________________________Our related services- ADMET- Biomarkers- Pharmacology
