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Takeda, Heptares probe GPCR’s role in CNS disorders
May 2011

OSAKA, Japan—Takeda Pharmaceutical Co. and Heptares Therapeutics on April 11 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.
According to the companies, 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.
Heptares will use its stabilized receptor (StaR) technology to engineer the first-ever thermally stabilized forms of the GPCR, and also apply advanced structural biology and rational drug design approaches to characterize 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.
"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, in a statement. "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 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," added Shigenori Ohkawa, chief scientific officer at Takeda. "The Heptares platform applies broadly to the GPCR target family and delivers stabilized forms that most precisely capture the pharmacological conformations of GPCRs as they exist in their natural cellular environments."
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 $2.8 million and an investment in an equity stake of approximately $4.6 million purchased by Takeda Ventures Inc., a wholly owned subsidiary of Takeda. Heptares is also eligible to receive future milestone payments of up to $98.5 million, 3 plus royalties on product sales. Further terms of the agreement were not disclosed.



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