Despite only being founded in 2007, Heptares Therapeutics has had an eventful short life. In early 2009 the company raised an impressive amount for a series A venture capital financing round, £21m ($30m), and followed that six months later with a research deal with the Novartis Option Fund, worth up to $200m.
What is attracting interest is Heptares’ work with G-protein couple receptors (GPCRs). Around a quarter of current small molecule drugs target GPCRs and as such they are a big area of interest for pharma companies. However in many disease areas these targets have proven difficult to hit. Heptares believes its technology can help discover more effective drugs to these previously intractable targets and hopes to find a partner by the end of this year to take its most advanced candidate, an adenosine A2A receptor antagonist, into the clinic.
Heptares has developed a GPCR stabilisation technology known as StaR (Stabilised Receptor), which enables the company to apply previously unavailable discovery techniques to GPCRs, including X-ray structure-based design, receptor binding kinetics analysis, fragment screening, and antibody generation.
The hope is the company can emulate the success seen with the discovery of novel drugs targeting soluble enzymes and radically improve the chances of discovering more effective drugs to these targets.
The most advanced candidate to emerge from the company’s lab so far is the A2A receptor antagonist programme, an area that has been widely researched for more than a decade, mostly in Parkinson’s disease, and a number of candidates are progressing through the clinic (Therapeutic focus - A2A antagonists lining up to enter final stage Parkinson's trials, April 22, 2010).
“Some of the later stage compounds look promising but there is still opportunity for a better compound,” Barry Kenny, chief business officer for Heptares, tells EP Vantage.
“We tried to identify a new compound using our novel discovery approach, and we believe we have a candidate ideal for CNS development.”
Dr Kenny says they are at the candidate selection phase and should be ready to nominate a high quality development compound, which is from a new chemical class, to take forward around mid year.
Toxicology issues have already derailed several A2As, but Heptares hopes to have overcome this issue with improved pharmacokinetics.
“We plan to find a partner before going into man, and would like to partner by the end of 2010. We are encouraged by the discussions,” he adds.
Interestingly, a couple of the companies talking to Heptares are not interested in the Parkinson’s indication, but the compound's broader CNS potential, particularly ADHD.
“Many bigger players don’t consider Parkinson’s a big enough opportunity,” Dr Kenny says.
As well as looking for a partner for the A2A programme, Heptares is also on the hunt for broader strategic research alliances, granting access to its discovery platform to interested parties. The company is already in “significant discussions” with a number of major pharma groups, Dr Kenny says.
“The platform has applications for small molecule and biologics in terms of antibody creation. This should be of significant interest to pharma partners.”
Interestingly, the company has decided that it has no interest in taking any of its compounds into man by itself.
“We think the value add is in the discovery stage where our technology is already identifying new chemical space for GPCR drug discovery. We have a pipeline of first-in-class and best-in-class molecules, that should attract interest,” Dr Kenny says.
Clearly, big pharma is already interested. As well as the research deal with Novartis Option Fund, under which Heptares will apply its StaR platform to generate drug leads against a particular GPCR target of interest to the Swiss pharma giant, the fund also invested £7m in the series A round.
Another alliance with a different big pharma name would certainly validate Heptares’ approach. Further successes will no doubt raise questions about how long the young company can remain independent given big pharma’s continued interest in new platform technologies.