Hypha Discovery: metabolite synthesis and purification specialists
WHAT'S NEW - Q3 2021
Late-stage chemical glucuronidation screens
Hypha's late-stage chemical glucuronidation screens have been hugely successful in producing acyl, N- and O-glucuronides of client drugs. For some difficult-to synthesise N-glucuronides, we have been able to provide a cost-effective solution to replace a mammalian biotransformation route.
The value of using multiple chemical screens is nicely exemplified through production of both an N- and O-glucuronide of posaconazole through scaling up the best conditions. The structures were elucidated by NMR spectroscopy.
Glucose conjugates
Although formation of glucoside drug conjugates is uncommon in humans, they appear more frequently as plant metabolites of pesticides.
Hypha have a number of techniques for making glucosides of drugs and agrochemicals. These comprise microbial biotransformation and a number of glucosyltransferases cloned from microbes in our collection. Our late-stage chemical synthesis techniques are also effective at making glucose conjugates.
Another happy client
We were delighted to receive this feedback from another satisfied client who needed glucuronides of two different compounds.
Originally the glucuronides had been observed in human hepatocyte incubations. We used two different techniques to make each glucuronide. Microbial biotransformation was used to make tens of milligrams of the target glucuronide of drug A, where only one microbe in the screening panel was able to produce the target. Production of the glucuronide of drug B was achieved by scaling up the best late-stage chemical synthesis conditions to generate hundreds of milligrams of the target glucuronide. It’s a great example illustrating the flexibility of the one-stop metabolite shop.
“The process of screening, scale-up and analysis of metabolites was truly seamless. We appreciated Hypha’s expertise and flexibility in providing us with different options to meet our needs.
They are a valuable partner for tackling any metabolite isolation questions and a pleasure to work with.”
Director of DMPK, Biotech company, Canada
METABOLITE TALES FEATURE
In this blog post we explore the metabolism of various drug structures that contain cyclopropyl groups, revealing that cyclopropyl groups can be used advantageously to diminish oxidative metabolism in some circumstances, but when coupled to amines can lead to potentially reactive intermediates. The story of risdiplam, the first oral drug to treat spinal muscular atrophy, is an especially interesting one!
Introducing Samuel Coe Ph.D
We're pleased to introduce Samuel Coe as Business Development Manager at Hypha. Sam is a medicinal chemist by training having previously worked in the pharma space for Vertex, Charnwood Molecular and Evotec.
Hypha's New Website
We launched our new website www.hyphadiscovery.com this summer. Check out the new Resources section which features our brochures, case studies, posters and publications as well as our new blog.
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.
