Drugging the Undruggable: New Acquisition to Boost GPCR Drugs

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Heptares Therapeutics has acquired G7 Therapeutics to take control over its GPCR technology, boost its pipeline and keep competitors in this profitable field at bay.

Heptares Therapeutics develops therapies directed to G protein-coupled receptors (GPCRs), a large family of hot but elusive targets for biopharma. The British company, owned by the Japanese Sosei, just announced it is acquiring G7 Therapeutics for €11M (CHF12M), which will become Heptares Zurich.

With this move, Heptares gets hold of G7’s technology platforms to rapidly generate stable GPCRs. These valuable molecules are the target of up to 30% of approved drugs and can hold the key to treating many diseases, ranging from Alzheimer’s to cancer. However, their conformational flexibility in solution is a huge challenge that leads most candidates to fail.

Heptares GPCR
Stabilized GPCR bound to its target

Heptares’ StaR technology addresses these problems by introducing mutations in GPCRs to stabilize the molecule without disrupting their biological activity. Now, the company incorporates G7’s SaBRE and CHESS platforms, which employ molecular evolution techniques to obtain a wide variety of GPCR variants that can be easily expressed in bacteria or yeast.

This acquisition will further boost Heptares’ pipeline, which already counts with multiple candidates for Alzheimer’s, schizophrenia, immuno-oncology, migraine, addiction and metabolic disease. Its lead candidate is currently in Phase Ib trials for cognitive impairment in Alzheimer’s and schizophrenia. With top-level partnerships with AstraZeneca, Kymab, MedImmune, MorphoSys, Teva, and billion-euro deals with Allergan and Pfizer, the company seems to be well-prepared to make a successful entry in the market.

Although many have failed after being lured into this profitable field, a few stand to give the British company a run for its money: Confo Therapeutics, born just last year in Brussels, is developing camelid antibodies to stabilize GPCRs in druggable conformations. Proteros, in Munich, also focuses on GPCRs and has signed up deals with MSD, Janssen, and Bayer. Hopefully for Heptares, its new GPCR platforms might give it the necessary push to keep its rivals behind.

Featured image by Kubicka/shutterstock.com; image from Heptares


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