Ensemble Therapeutics Forms Global Strategic Collaboration for Development of Oral, Macrocyclic IL-17 Antagonists and Additional

  Ensemble Therapeutics Forms Global Strategic Collaboration for Development
  of Oral, Macrocyclic IL-17 Antagonists and Additional Disease Targets

 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

Business Wire

CAMBRIDGE, Mass. -- August 6, 2013

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.

Contact:

The Yates Network
Gina Nugent, 617-460-3579
gina@theyatesnetwork.com