Ensemble Therapeutics Presents Data Demonstrating Unique Properties of Synthetic Macrocycles for Pursuing Challenging Targets

Ensemble Therapeutics Presents Data Demonstrating Unique Properties of Synthetic Macrocycles for Pursuing Challenging Targets

February 13, 2013

Preclinical Data Showing Benefits of Macrocycle Discovery Platform in Identifying First-in-Class Oral IL-17 Antagonists Presented At Molecular Med Tri Con 2013 Conference

CAMBRIDGE, Mass.--()--Ensemble Therapeutics today announced that preclinical data showing the advantages of novel macrocyclic compounds against challenging drug targets, including its first-in-class, orally active small molecule antagonists of IL-17, will be presented at the Molecular Med Tri Con 2013 Conference being held February 11-15, 2013 in San Francisco, CA.

“Our data demonstrate that Ensemble’s DNA-Programmed Chemistry discovery platform rapidly and successfully identifies novel, orally active small molecules against ‘undruggable’ targets that have historically proven intractable to traditional small molecule efforts, including protein-protein interaction targets like IL-17,” said Dr. Michael D. Taylor, CEO of Ensemble Therapeutics. “IL-17 is a clinically validated target previously impervious to traditional small molecule pharmaceutical approaches and has only been addressed to date with injectable protein therapeutics. Ensemble has discovered macrocycles that bind to IL-17 and have oral bioavailability and oral efficacy in animal inflammatory disease models.”


  • ‘Moving In New Circles – An Introduction to Macrocycles in Drug Discovery’, Nick K. Terrett, Ph.D. - Chief Scientific Officer, Ensemble Therapeutics, Wednesday, February 13, 2013, 12:10pmPT, Session: Mastering Medicinal Chemistry in an Era of Tough Targets
  • ‘The Solution to "Tough-to-Drug" Targets: An Integrated Discovery Engine Leveraging the Unique Properties of Synthetic Macrocycles’, Stephen Hale, Ph.D., Vice President, Drug Discovery, Ensemble Therapeutics, Friday, February 15, 2013, 9:05amPT, Session: Hot Targets to Watch: Protein-Protein Interaction Targets

About Ensemblins

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.

About Ensemble Therapeutics

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: www.ensembletx.com.



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Gina Nugent, 617-460-3579