MRC spin-out Heptares shines light on UK biotech

Funding

Heptares Therapeutics Ltd, a 2007 spin out from the UK Medical Research Council’s Laboratory of Molecular Biology in Cambridge, has lifted the gloom around UK biotech by raising £21 million in its first formal funding round.

The drug discovery company specialises in drugs targeting G-protein-coupled receptors (GPCRs), and has a platform technology which enables it to work with previously intractable members of this important class of receptors. Around 25 per cent of marketed drug are targeted at GPCRs.

Clarus Ventures led the syndicate, which includes the founding investor, MVM Life Science Partners, and the Novartis Option Fund. All three investors contributed equally. MVM previously provided two rounds of seed funding, allowing the company to develop and validate its technology.

The money will fund Heptares over the next three years to develop its own pipeline of small-molecule drug candidates using its proprietary StaR (Stabilised Receptor) technology platform. These will be developed against currently intractable GPCRs that are highly validated targets for the treatment of disease. The company will focus on metabolic and central nervous system disorders as areas of unmnet medical need where its technology has particular potential, and expects to partner in other areas, for example, therapeutic antibodies against GPCRs.

GPCRs play a crucial role in many diseases and are the site of action of 25-30 per cent of current drugs. As such they represent a major area of interest for pharmaceutical companies. However, these membrane proteins are notoriously difficult to isolate from cells in an intact and active form, and this has severely restricted efforts to study GPCRs using high throughput drug discovery techniques.

Heptares is able to engineer and purify GPCRs in stable and functional conformations that retain their drug-binding characteristics, allowing it to apply discovery tools such as crystallisation and structure-based design, biophysical analysis of ligand interactions, and fragment screening to stabilised GPCRs. This is expected to radically improve the chances of finding drugs to previously intractable targets and enable the development of safer and more selective therapeutic agents.

In 2008 the StaR technology was validated when it was used to elucidate the three-dimensional atomic resolution structure of the beta-1 adrenergic receptor, which is the site of action of beta blockers.

Heptares’ CEO, Malcolm Weir, said, “We are very pleased to have completed this significant fundraising in the current economic environment. We now have a very good opportunity to implement our strategy for generating new drug candidates to highly validated but previously challenging GPCRs.”

Michael Steinmetz, Managing Partner at Clarus Ventures, said, “Heptares has made impressive progress in developing its unique StaR technology since its inception in 2007.  Its platform has the potential to make important GPCR drug targets accessible to drug discovery techniques previously not applicable to this class of proteins. The commercial opportunity arising from developing new first/best-in-class drugs to GPCRs is clear, particularly with pharmaceutical company pipelines under pressure.”