Coupling their efforts on promising G-protein coupled receptor

Heptares and Takeda Pharmaceutical initiate drug discovery collaboration focused on GPCR linked to CNS disorders

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CAMBRIDGE, England—Heptares Therapeutics and Japanese pharma giant Takeda Pharmaceutical Co. 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 (CNS) disorders. They say that 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.

However, they are pursuing this GPCR target because, the companies say, "A new medicine targeting this GPCR would be first-in-class."

Under the terms of the deal, Takeda gets worldwide commercial rights to new drugs emerging from the collaboration. Upon signing, Heptares receives an upfront payment of about $2.7 million and an investment in an equity stake of approximately $4.5 million purchased by Takeda Ventures Inc., a wholly-owned subsidiary of Takeda. Heptares is also eligible to receive future milestone payments of more than $96 million 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," says 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."

To carry out the work of the collaboration, Heptares will put its proprietary StaR (stabilized receptor) technology to work to engineer the first-ever thermally stabilized forms of the GPCR as the basis for the drug discovery program. Heptares will also apply advanced structural biology and rational drug design approaches to characterize the GPCR's structure and to generate early leads. Takeda will take part in lead generation and ultimately assume responsibility for preclinical and clinical development of new drugs candidates.

"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," says Shigenori Ohkawa, chief scientific officer at Takeda. "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."

Since its inception, Heptares has raised more than $35 million from venture capital firms like Clarus Ventures, MVM Life Science Partners and Novartis Option Fund. The companies' officials say that GPCRs represent the single most important family of drug targets in the human body, but lament that because of their inherent instability when removed from cell membranes, little or no structural information about these targets has been available to drive structure-based drug discovery programs.

Heptares sees its StaR technology as the trailblazer to enable the first-ever thermo-stabilization of GPCRs, a breakthrough Heptares says allows its researchers "to resolve GPCR structures and deploy structure-based drug discovery techniques to identify potent and selective drug candidates to previously undruggable targets."

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