A pair of GPCR deals for Q1

Heptares inks agreements with Daiichi Sankyo and University of Cambridge centered on GPCRs

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LONDON—The first quarter of the year hadn’t closed before Heptares Therapeutics, a wholly owned subsidiary of Sosei Group Corp., announced two deals focused on G protein-coupled receptors (GPCRs), a superfamily of 375 receptors that are implicated in a variety of diseases.
The first such deal was signed with Daiichi Sankyo. Per the terms of the agreement, Daiichi Sankyo will gain exclusive global rights for the development, manufacture and commercialization of Heptares-discovered novel small molecules, for which it will pay $4 million in an upfront payment and approximately $8 million in research funding. Heptares also stands to receive additional research, development and commercialization-based milestone payments as well as royalties on net sales of products resulting from the agreement.
As noted in a Daiichi Sankyo press release, Heptares will leverage its StaR technology “to engineer thermally stabilized forms as the basis for the drug discovery program. Heptares will also employ advanced structural biology and rational drug design approaches, X-ray crystallography and fragment screening to delineate the GPCR’s structure and to generate lead candidates.” For its part, Daiichi Sankyo will play a role in lead generation and in-vivo models. The companies will be focusing on a GPCR chosen by Daiichi Sankyo that is known to play a role in pain relief.
“This is a very exciting new collaboration as relieving pain presents a significant challenge,” Malcolm Weir, CEO of Heptares and chief R&D officer of Sosei, commented in a statement. “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.”
The Daiichi Sankyo deal came just over a month after Heptares shared news of another research collaboration, this one with the University of Cambridge. The program will run three years, and Heptares will work with Dr. Anthony Davenport and his group at the Department of Experimental Medicine and Immunotherapeutics at the university. The team’s focus will be on discovering novel molecules that can target and modulate the apelin receptor, a GPCR found on the surface of cells in the lung, heart and vascular system. This receptor has been implicated in several cardiovascular diseases.
“We have made great strides in recent years to increase our understanding of the role of the apelin receptor system and its involvement in cardiovascular diseases. It is an exciting target and we are delighted to be advancing this research with Heptares to better understand the role of apelin and related peptides with a view to informing the optimal way of targeting the apelin system for treating cardiovascular diseases,” Davenport stated in a press release.
Heptares’ ORBIT initiative was launched in February 2016 as a collaborative research effort aimed at promoting and broadening the application of its proprietary structure-based drug design experience with GPCRs in pursuit of new medicines. The company intends to commit up to £5 million (approximately $6.2 million) to this effort over the next three years. Under the auspices of ORBIT, Heptares will collaborate with leading academic groups and emerging biotechnology companies to search for links between GPCRs and disease as well as how GPCR targets relate to disease biology. In addition to the collaboration with the University of Cambridge, Heptares has also begun an ORBIT program with Imperial College London’s National Heart and Lung Institute targeting an orphan receptor implicated in several immune disorders, such as asthma and inflammatory bowel disease.
Fiona Marshall, chief scientific officer of Heptares, said: “The collaboration with Dr. Davenport’s group is a great example of how the ORBIT program supports our strategy to expand the reach of our technology to new targets, in particular through an investment in translational medicine and understanding the role of GPCRs through studies on human tissues. The apelin receptor is emerging as an exciting new target in the regulation of cardiovascular function and offers a unique approach to treat a number of serious cardiovascular diseases.”

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