Collaboration to Accelerate Ensemble’s Novel, Oral, Interleukin-17 Inhibitor Program, and to Leverage Ensemble’s Innovative Drug Discovery Chemistry Platforms Against Certain Other Targets

CAMBRIDGE, MA, USA I August 6, 2013 I Ensemble Therapeutics, a biotechnology company developing Ensemblins™, a novel class of small molecule therapeutics with the power of biologics, today announced the initiation of a two-part research and development collaboration with Novartis. The companies have entered into a strategic development agreement for Ensemble’s most advanced proprietary program that targets the inflammatory cytokine IL-17, and for a new program to discover novel small molecule treatments against undisclosed drug targets specified by Novartis using Ensemble’s proprietary drug discovery platforms.

Under the terms of the agreement, Ensemble will receive an undisclosed upfront payment from Novartis and is also eligible to receive potential success-based development and sales milestone payments. In addition, Ensemble will receive tiered royalties on potential future sales of products that may arise from the collaboration. Novartis will also provide research funding to Ensemble during the term of the collaboration.

“We are very pleased to enter into this collaboration with Novartis, a clear leader in the development of treatments for IL-17-dependent inflammation and autoimmune diseases,” said Ensemble CEO Michael D. Taylor, PhD. “Novartis has recognized the strength of Ensemble’s orally bioavailable drug candidates against this difficult-to-drug protein:protein interaction target, and we believe Novartis is the best-suited pharmaceutical company to partner with us to rapidly develop and market important new medicines for the treatment of IL-17-mediated disease,” he continued. “The discovery component of our alliance reinforces the mutual commitment to advance candidates from Ensemble’s macrocycle-based chemistry.”

Ensemble’s class of IL-17 antagonists licensed by Novartis represent the potential for first-in-class, orally active, small molecule inhibitors of this important, clinically-validated target. The protein-protein nature of interaction of IL-17 with its receptor has made design of traditional small molecule pharmaceutical inhibitor difficult, so has been addressed to date with injectable protein therapeutics directed to the ligand. An orally-active inhibitor of IL-17 would have a profile complementary to the current class of clinical stage anti-IL-17 antibody products, which have shown compelling efficacy in multiple human clinical trials involving various inflammatory and autoimmune diseases.

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. Prior to this agreement, Ensemble entered high-value partnerships including alliances with Boehringer Ingelheim, Genentech, Bristol-Myers Squibb, Alexion Pharmaceuticals 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 by the end of 2013. For more information, visit: www.ensembletx.com.

SOURCE: Ensemble Therapeutics