Hypha’s Q3 2016 Newsletter – Parallel production of major human metabolites from diverse metabolism of epacadostat to support clinical drug development
Hot-off-the-press news describing the scale-up of human metabolites resulting from mixed metabolism of Incyte’s first-in-class IDO1 inhibitor epacadostat (EPA) is the topic of our newsletter for Q3. EPA is currently in Phase III clinical trials in combination with Merck’s pembrolizumab for treatment of metastatic melanoma.
EPA, an orally available hydroxyamidine, has an interesting mechanism of metabolism, resulting in 3 major circulating metabolites comprising a glucuronide, gut metabolite and a secondary CYP derived structure. Biocatalysis of EPA using Hypha’s microbial panel provided a route to achieve formation of all three human metabolites.
More information on this topic, including the reference to a publication in Drug Metabolism and Disposition on EPA metabolism, can be found in our newsletter for this quarter via the link below: