Production of a glucuronide metabolite of praliciguat by microbial biotransformation
Great to see Hypha recognised for producing a glucuronide metabolite of praliciguat (M3) in the paper just out in the journal Pharmacology Research & Perspectives.
There are several pathways involved in the metabolism of praliciguat in rats, including oxidation, reduction, dealkylation, sulfation, glucuronidation and glutathione conjugation. Praliciguat-glucuronide (M3) is the most abundant single metabolite in bile.
Microbial biotransformation is an efficient and scalable method for producing O-glucuronides and other metabolites of drug candidates. In this client project, nearly 100% of praliciguat was biotransformed to a single O-glucuronide by one of Hypha’s biotransforming microbes to provide a total of 184 mg of purified praliciguat-glucuronide at > 99% purity. The material enabled the structural elucidation of the position of the glucuronide conjugate and was used for determining the identification and circulating concentrations of this metabolite in clinical samples.
The paper is open access at https://bpspubs.onlinelibrary.wiley.com/doi/10.1002/prp2.579