AstraZeneca plc and Heptares Therapeutics Ltd have agreed a four-year collaboration in which they will work on the discovery and development of drugs targeting G-protein coupled receptors (GPCRs).
GPCRs are among the largest and most important family of proteins found in the human body and represent the single most important class of drug targets. However, due to 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 programmes.
Under the terms of the agreement, AstraZeneca has worldwide commercial rights to product candidates emerging from the collaboration. Heptares will receive a $6.25 million upfront payment, plus R&D funding and will then be eligible for $181.75 million in possible milestone payments and royalties on the sale of any products.
This collaboration brings together Heptares’ GPCR discovery expertise and proprietary technologies, including its StaR technology, through which it engineers stabilised GPCR receptors, with AstraZeneca’s discovery, development and commercialisation capabilities.
The research will focus on a number of specific GPCR targets linked to central nervous system/pain, cardiovascular/metabolic and inflammatory disorders. It will provide the starting point for drug discovery by producing the first-ever stabilised forms of the GPCRs nominated by AstraZeneca This will make these targets amenable to high throughput screening and other advanced drug discovery techniques.
Heptares and AstraZeneca will engage their discovery teams, compound libraries, and other discovery technologies for initial screening and lead identification. Results will be combined into a common pool and the best leads will be further optimised collaboratively. AstraZeneca will then select pre-clinical, small molecule and antibody candidates and will be solely responsible for preclinical and clinical development.
“This alliance with AstraZeneca illustrates the broad power and scalability of the Heptares technology to generate novel drug candidates in regions of GPCR space that were previously regarded as closed to pharmaceutical discovery,” said Malcolm Weir, CEO of Heptares.
Since it was formed around technology from the UK Medical Research Council National Institute of Medical Research in London and its Laboratory of Molecular Biology in Cambridge in 2007, Heptares has raised more than $35 million from venture investors, Clarus Ventures, MVM Life Science Partners and Novartis Option Fund, and has formed partnerships with Shire, Takeda, and Novartis.
Receive our Policy Bulletin each Tuesday & Thursday and news about bridging Europe’s east-west innovation gap twice a month in The Widening. 
