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Home - Sosei Heptares
A world-leader in GPCR medicine design and development
Updated 07 Jul 2026 09:49
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Heptares Therapeutics is a drug discovery company focused on the discovery of novel small-molecule drugs targeting G-protein coupled receptors. Drawing on pioneering work at MRC LMB and MRC NIMR, it has developed novel stabilisation technology (StaRTM) to render these and other difficult drug targets susceptible to structural analysis by X-ray crystallography and complementary biophysical methods. They can also be used as antigens for the development of therapeutic antibodies. In February 2015, Heptares became a fully-owned subsidiary of Sosei Group Corporation. www.heptares.com
The structure of a beta1 adrenergic receptor was solved by X-ray crystallography in 2008 using this approach. In 2011, structures of the A2A adenosine receptor both complexed with antagonists, and, for the first time for any GPCR, with the endogenous agonist were also solved, the latter by my ex post-doc, Guillaume Lebon. Arising from the A2A work, a best-in-class selective antagonist has been developed that has been licensed to Shire pharmaceuticals. StarTM technology has so far proved to be generically applicable to GPCRs, and is causing much excitement within the pharmaceutical industry and the wider GPCR community. More than 7 other GPCRs are in the StaR pipeline. Successful applications of StarTM technology in 2012-2015 have included the Orexin-1 receptor, the M1 muscarinic acetylcholine receptor complexed with novel selective agonists, the corticotrophin releasing factor 1 receptor and the transmembrane domain of the mGluR5 receptor. Heptares scientists have confirmed the novel mode of interaction of selective agonists of the M1 muscarinic receptor first proposed as a result of work in my laboratory. These structures are feeding into the development of novel drug candidates directed at these and related receptors for a number of important clinical situations including type 2 diabetes, migraine, addiction and compulsive disorders, chronic insomnia, anxiety and depression, autism and cognitive enhancement. In February 2016, Heptares reported a successful phase 1b clinical trial of a first-in-class selective M1 mAChR agonist designed to enhance cognition in dementia and schizophrenia, devoid of parasympathetic side effects. Heptares Therapeutics is a world-leader in structure-based drug design.
1 Apr 2015 to 31 Mar 2018
Congenital Hyperinsulinism is a rare neonatal disease presenting severe hypoglycaemia associated with poor clinical outcomes and long-term neurodisability. The support of the Technology Strategy Board will enable Heptares, in collaboration with the University of Manchester and Great Ormond Street Hospital, to carry out the pre-clinical development of a no...
