Ensemble Therapeutics to Present Data on IL-17A Inhibitors that are Novel, Oral Macrocycles Against Previously Undruggable Target

Ensemble Therapeutics to Present Data on IL-17A Inhibitors that are Novel, Oral Macrocycles Against Previously Undruggable Target

The Yates NetworkGina Nugent, 617-460-3579

Ensemble Therapeutics today announced that preclinical data showing the advantages of its Ensemblins, novel macrocyclic compounds against challenging drug targets, will be presented at the 245th American Chemical Society (ACS) National Meeting being held April 7-11, 2013 in New Orleans, LA. In particular, the presentation will highlight Ensemble’s first-in-class, orally active small molecule antagonists of Interleukin-17 (IL-17), a cytokine implicated in multiple inflammatory and autoimmune diseases, and present preclinical data on the oral efficacy and anti-inflammatory effects of the company’s IL-17A inhibitor Ensemblin.

“Ensemble’s DNA-programmed chemistry platform rapidly screened and identified novel, orally active small molecules against IL-17, a key pro-inflammatory cytokine known to be active in human and animal models of rheumatoid arthritis,” said Dr. Michael D. Taylor, CEO of Ensemble Therapeutics. “Ensemble's small molecule IL-17 antagonists retain certain attractive DMPK characteristics such as extended duration of target binding — measured in hours and comparable to the IL-17 biologics currently in development -- and also desirable drug-like properties including oral bioavailability and demonstrated oral efficacy in animal models.”

Ensemble will also be presenting on its first-in-class, orally active small molecule antagonists of Interleukin-17 at the CHI Drug Discovery Chemistry conference on April 16, 2013 in San Diego during the Constrained Peptides and Macrocyclics Drug Discovery session: /

Ensemblins™ are a new class of synthetic macrocycles developed by Ensemble using its proprietary chemistry platforms, including DNA-Programmed Chemistry. Macrocyclic rings are found in many natural product-based drugs and bestow favorable pharmaceutical properties and powerful protein surface binding properties upon such drugs. Thus, macrocycles are uniquely suited to address many protein targets that cannot be modulated effectively by traditional small molecule pharmaceutical compounds. Macrocycles have been challenging to synthesize in large numbers and this has constrained their wider use in the industry. By extending beyond the limits of traditional small molecule drug discovery, Ensemble’s platform provides unmatched capabilities to successfully and reliably generate millions of macrocyclic Ensemblins as drug candidates, larger than any collection previously synthesized in the pharmaceutical industry.

Based in Cambridge, MA, Ensemble Therapeutics is deploying its proprietary chemistry platforms to develop a novel class of therapeutics known as “Ensemblins”. Ensemble is leveraging its macrocycle drug discovery expertise to fuel its proprietary drug candidate pipeline while also pursuing collaborations with pharmaceutical partners. Ensemble has entered high-value partnerships including alliances with Boehringer Ingelheim, Genentech, Bristol-Myers Squibb and Pfizer to access Ensemble’s macrocycle libraries for purposes of affinity screening drug discovery against difficult-to-address targets. Ensemble’s internal discovery and development efforts are focused on the key therapeutic areas of oncology and immuno-inflammatory diseases, with its lead program, a small molecule antagonist of Interleukin-17, a cytokine implicated in multiple inflammatory and autoimmune diseases, poised to enter development with an orally active candidate in 2013. For more information, visit: .

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