Hypha Discovery: metabolite synthesis and purification specialists

 
 

WHAT'S NEW

 
 

N-glucuronides: on the rise?

We’ve observed an increase in synthesis requests for N-glucuronides over the last few years. We speculate that this may be due to the growing inclusion of nitrogen containing heterocycles in the design of new small molecule drugs, and pan company strategies to reduce CYP metabolism.

The situation is further complicated by the high interspecies variability in formation of some N-glucuronides, especially aliphatic tertiary amines and aromatic N-heterocycles. 

UGT1A4 and UGT2B10 are key enzymes responsible for N-glucuronidation reactions in humans, rates of which can be much higher than in other animals.

To compound this, synthesis of N-glucuronides isn’t always straightforward - read about Hypha's solutions to accessing and characterising N-glucuronides here.

N-glu synthesis solutions
 

More great client feedback

We've received some more feedback for the excellent work Hypha scientists did to ensure successful completion of a challenging metabolite project for a US pharma client. 

“Hypha Discovery was a huge help to our drug development timeline, when an ADME study revealed significant metabolites that were challenging to synthesize chemically. Hypha was able to rapidly reproduce the metabolites to confirm chemical structure, and then scale up to support nonclinical testing and bioanalytical method development, with far greater speed than chemical synthesis could achieve. The Hypha people were very pleasant to work with and the material they produced was of very high quality, which rounded out an overall great experience. I would recommend them without reservation.”

Senior VP Pharmaceutical Sciences, US Pharma company

 
 
 

LEARN MORE

 
 
 

Metabolite synthesis and characterisation

On the move

Hypha contributed a chapter on “Metabolite Generation and  Characterization by NMR” in the 2020 book  on "Identification and Quantification of Drugs, Metabolites, Drug Metabolizing Enzymes and Transporters."

 

Impact of Biotransformation

Biotransformation in drug discovery

Read our Innovations article in ACS Med. Chem. Lett. addressing the impact of metabolism and leveraging biotransformation to deliver improved drug leads.  “Biotransformation: Impact and Application of Metabolism in Drug Discovery”  

Link to paper
 

Late-stage hydroxylation

Watch our last webinar on "Hydroxylating drugs, why bother?",  featuring the application of PolyCYPs enzymes for late-stage hydroxylation of lead compounds. Contact us for a link to a recording.

Contact Us
 

About Hypha

Hypha are experts in the scalable synthesis, purification and structure elucidation of metabolites of drugs and agrochemicals. We work with pharma and agrochemical companies worldwide to fulfil our clients' needs to obtain metabolites for definitive MetID and for further biological testing. Applying a comprehensive portfolio of methods, including microbial and liver S9 / microsomal biotransformation methods, chemical synthesis, and recombinant enzymes, Hypha has the ability to produce gram amounts of synthetically challenging metabolites and oxidised derivatives of drugs. Combined with strong capabilities in purification chemistry and structural elucidation using state-of-the-art NMR spectroscopy, we are able to deliver an end-to-end service to clients.

 
 
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Hypha Discovery Limited,
154B Brook Drive, Milton Park, Abingdon, OX14 4SD, UK
www.hyphadiscovery.co.uk
Email us at enquiries@hyphadiscovery.co.uk
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