Heptares is a pioneer in the discovery of new medicines targeting G-protein-coupled receptors (GPCRs), a super-family of proteins linked to many human diseases. Leveraging its deep GPCR expertise and a revolutionary discovery engine, Heptares has built a powerful and fully-integrated drug discovery platform enabling it to generate a pipeline of first-in-class and best-in-class GPCR-targeted medicines, focused on CNS and metabolic indications.

The Heptares technology platform provides unprecedented insight into GPCR biology enabling the design of novel drugs that selectively modulate clinically important, yet historically intractable, GPCR drug targets. This represents a unique GPCR capability in the industry today, opening up new possibilities for both small molecule and antibody therapeutics across the GPCR target universe.

Heptares is the first and only company transforming GPCRs, which are typically highly unstable when removed from cellular membranes, into stabilised receptors or StaRs®. StaRs® enable GPCR structures in their natural pharmacological conformations to be determined, thereby overcoming a major historical barrier to structure-based GPCR drug discovery. Heptares has also invented BioPhysical Mapping™, which provides superior elucidation of GPCR-ligand interactions, and has engineered new fragment-based and in silico technologies specifically tailored to GPCR lead discovery and optimisation.

Heptares has raised over $40 million from leading life science investors and has formed strategic alliances with AstraZeneca, MedImmune, Shire, Takeda and Novartis.

Latest News

Jan 25, 2012

Heptares’ Patents Covering Stabilised Receptor (StaR®) Technology Granted in Europe and Japan

Key patent grants protect Heptares’ leading position in GPCR-targeted drug design and discovery

Jan 25, 2012

Heptares Scientists Report The First Use of Structure-Based Design to Discover GPCR-Targeted Drug Candidate