Heptares Therapeutics Ltd is looking to out-license its most advanced programme, which is focused on the adenosine A2A receptor, a clinically validated target for the treatment of Parkinson’s disease.
The company has identified a number of potent and selective small molecule antagonists by virtual screening and in-house structure-based design, from which a lead candidate is being progressed to preclinical development. Heptares now wants to out-license the programme, having advanced it to this stage from initiation in only 18 months, a speed which it says reflects the power and efficiency of its approach for generating leads against G-protein-coupled receptor (GPCR) targets.
Heptares was founded in 2007 as a spin-out from the UK Medical Research Council to develop and commercialise a technology platform for stabilising GPCRs in functionally relevant conformations that retain their drug-binding characteristics. This allows the company to use advanced drug discovery technologies including X-ray structure-based design, fragment screening, and antibody generation.
The ability to do this is a significant advance because although they are acknowledged to be extremely important drug targets and many marketed drugs target these receptors, GPCRs are membrane-bound proteins and previously have proven very difficult to manipulate.
To date, Heptares has created more than 20 leads to more than 12 validated GPCR targets and is advancing multiple discovery programmes in central nervous system diseases, metabolic diseases and cancer.
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