Routes for Synthesis of Metabolites of Ruxolitinib and Epacadostat

Presented at: Drug Discovery Chemistry, April 2022

Routes for Synthesis of Metabolites of Ruxolitinib and Epacadostat

Abstract: Significant metabolites of small molecule drugs sometimes need to be accessed at scale for further testing. Hypha have developed multiple techniques as part of their one-stop metabolite shop to tackle synthesis of these using both biotransformation techniques or late-stage chemical synthesis.

In this poster we describe the routes taken to make metabolites of Incyte’s drugs, ruxolitinib and epacadostat, where the majority of metabolites were not accessible through facile chemical synthesis. Instead, microbial biotransformation was used to make the phase 1 and phase 2 metabolites needed.