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Heptares and Takeda Pharmaceutical Co. Ltd. (TKDG.DE) Initiate Drug Discovery Collaboration Focused on GPCR Linked to CNS Disorders; Heptares to Get GBP 4.5 Million Upfront and Up to GBP 60.5 Million  
4/11/2011 7:15:18 AM

CAMBRIDGE, England, April 11, 2011 /PRNewswire/ -- Heptares Therapeutics and Takeda Pharmaceutical Company today announced the formation of a two-year drug discovery collaboration focused on a single G-protein coupled receptor (GPCR) that plays an important role in the pathology of central nervous system disorders. This GPCR has proved intractable using historical drug discovery efforts, due to its instability when removed from cell membranes and the resulting lack of insight into its structure. A new medicine targeting this GPCR would be first-in-class.

During the collaboration, Heptares will leverage its proprietary StaR(R) (stabilised receptor) technology to engineer the first-ever thermally stabilised forms of the GPCR as the basis for the drug discovery programme. Heptares will also apply advanced structural biology[*1] and rational drug design approaches[*2] - including Biophysical Mapping(TM), X-ray crystallography and fragment screening - to characterise the GPCR's structure and to generate early leads. Takeda will participate in lead generation and then assume responsibility for preclinical development and clinical development of new drugs candidates.

Under the terms of the agreement, Takeda receives worldwide commercial rights to new drugs emerging from the collaboration. Upon signing, Heptares received an upfront payment of GBP1.7 million and an investment in an equity stake of approximately GBP2.8 million purchased by Takeda Ventures Inc., a wholly-owned subsidiary of Takeda. Heptares is also eligible to receive future milestone payments of up to GBP60.5 million[*3] plus royalties on product sales. Further terms of the agreement are not being disclosed.

"We are excited to be collaborating with Takeda to unlock a key GPCR target for treating CNS disorders, an area of significant unmet medical need where Takeda has established a leading scientific and commercial position," said Malcolm Weir, CEO of Heptares Therapeutics. "As we advance Heptares' internal pipeline of GPCR-targeted medicines, we also plan to pursue attractive external opportunities, such as this partnership with Takeda, to extend our technology broadly across the GPCR universe."

"The Heptares StaR(R) technology is a powerful new capability for discovering GPCR-targeted drugs and we look forward to applying it to a specific GPCR target of interest to Takeda in the area of neuroscience," said Shigenori Ohkawa, Chief Scientific Officer at Takeda Pharmaceutical Company. "The Heptares platform applies broadly to the GPCR target family and delivers stabilised forms that most precisely capture the pharmacological conformations of GPCRs as they exist in their natural cellular environments."

[*1] Structural biology is the combined use of molecular biology and biophysical technologies, in particular X-ray crystallography, for the elucidation of three-dimensional structures of biological macromolecules, especially proteins.

[*2] Rational drug design approaches apply structural biology to understand in atomic detail how compounds interact with their target receptors, so they can be systematically turned into viable drug candidates by iterative medicinal chemistry.

[*3] For future milestone payments, Heptares is eligible to receive GBP1M (GBP) in research-stage milestones and $96M (USD) in additional later-stage milestones. To report the total future milestone payments in the single currency of GBP, the figure reported above of GBP60.5M reflects the conversion of $96M at a current exchange rate of 0.62, which equals GBP59.5M (GBP), plus GBP1M (GBP), which equals GBP60.5M (GBP).

About Heptares Therapeutics

Heptares is a drug discovery company creating new medicines targeting G-protein-coupled receptors (GPCRs). The Company is currently leveraging its GPCR expertise and proprietary StaR(R) technology to build a pipeline of best-in-class and first-in-class GPCR-targeted medicines for the treatment of CNS, metabolic and other diseases.

GPCRs represent the single most important family of drug targets in the human body, yet, due to their inherent instability when removed from cell membranes, little or no structural information about these valuable targets has been available to drive structure-based drug discovery programmes. Heptares' StaR(R) (Stabilised Receptor) technology enables the first-ever thermo-stabilisation of GPCRs. This breakthrough allows Heptares scientists to resolve GPCR structures and deploy structure-based drug discovery techniques to identify potent and selective drug candidates to previously undruggable targets.

Heptares has raised more than $35 million from leading venture investors, Clarus Ventures, MVM Life Science Partners and Novartis Option Fund.

http://www.heptares.com

About Takeda Pharmaceutical Company

Located in Osaka, Japan, Takeda is a research-based global company with its main focus on pharmaceuticals. As the largest pharmaceutical company in Japan and one of the global leaders of the industry, Takeda is committed to strive towards better health for patients worldwide through leading innovation in medicine. Additional information about Takeda is available through its corporate website, http://www.takeda.com.

Contact Information:

Heptares Therapeutics Ltd +44(0)1707-358-629 Dr Malcolm Weir, CEO malcolm.weir@heptares.com Dr Barry Kenny, CBO barry.kenny@heptares.com Citigate Dewe Rogerson (For Heptares) +44(0)20-7282-2948 Dr Mark Swallow, Dr Chris Gardner mark.swallow@citigatedr.co.uk Takeda Pharmaceutical Company Mihoko Shinomiya +81-3-3278-2037

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