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).