Ensemble has identified a series of unique macrocycle small molecules, or Ensemblins, that are antagonists of Interleukin-17, a pro-inflammatory cytokine implicated in multiple inflammatory and autoimmune diseases such as psoriasis, rheumatoid arthritis, Crohn’s and intestinal bowel disease. These Ensemblins represent first-in-class small molecule antagonists of this important, clinically validated protein-protein-interaction target that has proven impervious to traditional small molecule pharmaceutical approaches and has only been addressed to date with protein therapeutics.  A small orally-active inhibitor of IL-17 would have significant delivery and therapeutic advantages over the current class of clinical stage anti-IL-17 antibody products. 

Ensemble knows of no other IL-17 small molecule antagonists, in spite of the active efforts of a number of major pharmaceutical and biotechnology companies to identify such compounds.  The discovery of a series of small molecule macrocycles that exhibit single-digit nanomolar potency, and are selective and druggable with excellent potential for oral administration, is a compelling example of the power of Ensemble’s drug discovery platform against a most challenging and significant drug target. The company expects this rapidly advancing IL-17 program to produce an orally active development candidate by the end of 2012.

[ back to top ]