Daiichi Sankyo and Heptares Therapeutics have established a drug discovery and licensing agreement to discover and develop small-molecule drug candidates that target a specific G protein-coupled receptor (GPCR), designated by Daiichi Sankyo, for potential applications in pain relief. Under terms of the deal Heptares, a Sosei Group subsidiary, will receive $4 million upfront, plus approximately $8 million in research funding, and additional research, development, and commercialization milestones. The U.K.-based firm will also be eligible for royalties on future sales of products developed as a result of the collaboration.

“This is a very exciting new collaboration as relieving pain presents a significant challenge,” said Malcolm Weir, Heptares CEO and chief R&D officer at Sosei. “We are confident that the unique structural insights of the receptor that our technologies can deliver combined with expertise on its role in pain from the neurosciences team at Daiichi Sankyo will yield new, differentiated molecules that can be advanced into development.”

Heptares is exploiting its StaR® (stabilized receptor) technology and structure-based drug discovery platform to develop a pipeline of drugs that target GPCRs. The firm’s lead M1 muscarinic receptor agonist, partnered with Allergan, is in Phase Ib development to address cognitive impairment in Alzheimer’s disease, schizophrenia, and other disorders. The broad potentially $3.3 billion R&D and commercialization agreement with Allergan signed in 2016 covers a number of Heptares’ subtype-selective muscarinic receptor agonists for treating neurological disorders, including an M4 agonist and dual M1/M4 agonists in preclinical development.

Heptares has additional drug development agreements in place with AstraZeneca, Teva, and Kymab. The firm received a $10 million milestone payment from AstraZeneca during mid-2016, when the oral adenosine A2A antagonist HTL1071/AZD4635 started in Phase I clinical development in patients with advanced solid tumors.

Heptares has ongoing technology partnerships with Pfizer, AstraZeneca, MedImmune, and Morphosys  focused on the discovery and development of small-molecule or antibody candidates against specified GPCR targets.

In January 2017, Heptares and the University of Cambridge, U.K., launched a 3-year research collaboration under Heptares’ ORBIT initiative to discover molecules that target the apelin GPCR for potential applications in cardiovascular disease. In November 2016, Heptares announced its $11.8 million acquisition of Swiss drug discovery and development firm G7 Therapeutics to strengthen its platform for GPCR drug design and development.

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