What We Do
Metabolite Synthesis
Synthesis of Metabolites of Drugs and Agrochemicals
Hypha are go-to experts in metabolite synthesis, purification and identification. We provide all types of phase I and phase II metabolites to small and large pharma and agrochemical companies globally.
We provide metabolites to clients for a variety of applications:
- Structure identification
- Authentic standards for bioanalytical method development
- Certified standards for clinical quantitative bioanalysis
- DMPK / Tox studies to satisfy regulatory guidelines, such as the FDA’s MIST guidelines and the EMA’s ICH guideline M3 (R2).
- Target / off-target activity testing
- Enzyme kinetic and intrinsic clearance assays
- For patent coverage and exploration of SAR
What We Do
Metabolites arising from a variety of pathways are accessible, including both CYP and non-CYP derived phase I mechanisms and phase II conjugates including all types of glucuronides.
We are typically asked to produce the following metabolite types:
- Oxidised metabolites
- CYP-mediated metabolites
- Non-CYP metabolites e.g. via AOX, FMOs
- Mixed phase I enzyme metabolites e.g. dihydrodiols resulting from the action of CYPs and epoxide hydrolase
- O-glucuronides
- Acyl glucuronides
- N-glucuronides
- N-carbamoyl glucuronides
- Sulfated metabolites
- GSH conjugates
- Gut metabolites resulting from metabolism by gut bacteria
- Mixed pathway or multi-step metabolites, e.g. hydroxylated/glucuronidated metabolites
- Stable-labelled and radiolabelled metabolites
Our “One-stop Metabolite Shop” concept comprises a comprehensive suite of technologies to enable scalable synthesis of even the most difficult-to-synthesise metabolites. Human and other mammalian phase I and phase II metabolites of drugs and agrochemicals can be synthesised using a variety of methods to maximise the chances of success, including chemical synthesis, mammalian biotransformation (S9s / microsomes of liver and other tissues), microbial biotransformation, recombinant enzymes such as PolyCYPs, as well as the purification of metabolites from biological matrices. Hypha scientists are also experts in structural elucidation and NMR spectroscopy.
Metabolites of agrochemicals
Key features
Phase I metabolites produced from both CYP and non-CYP mediated pathways, including via aldehyde oxidase and FMOs
Production of Phase II conjugates, including N- , O- &
acyl glucuronide and sulfated metabolites
Multiple metabolites can be captured in a single screen
Applicable to broad structural types and complex molecules
Solutions for synthetically challenging metabolites
Provides a tool for MetID and for accessing larger quantities of metabolites for further biological characterisation to satisfy regulatory requirements
Reproducible and scalable process to gram quantities
Formulation know-how for poorly-soluble compounds
Tailored project design and stage-gated payment structure
Simple fee for-service basis, i.e. there are no downstream terms or royalties
Resources
Explore our library of resources comprising brochures, case studies, posters and publications about the work we do.
In this open access review in Drug Discovery Today we look at the why, when and how metabolites of small-molecule drugs are synthesised from the perspective of a specialist CRO.
Access a brochure on how we make and characterise oxidised and conjugated metabolites of agrochemical compounds.
Interested in metabolite synthesis? Download this useful resource on how Hypha approach making metabolites of drugs and agrochemicals, featuring a variety of interesting case studies.
Find out about our related services
Hypha has exceeded our expectations and is now a ‘go to’ lab for biosynthesis/synthesis/purification. Hypha’s team was a pleasure to work with and our complicated projects were handled with expertise and professionalism. Their excellent scientific communication and project data were extremely comprehensive and we received updates throughout the process. We will definitely be Hypha Discovery clients for life
Director of DMPKHead of Toxicology
DMPX, US Pharma Company
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Hypha Discovery is a UK-based CRO supporting pharmaceutical and agrochemical companies worldwide through the production of metabolites and new derivatives of drugs and agrochemicals in discovery and development.