Convergence initiates CNV1014802 Phase II study in lumbosacral radiculopathy

Convergence Pharmaceuticals Limited ("Convergence"), the company focused on the development of novel and high value analgesic medicines, today announces that the Phase II proof of concept study with CNV1014802 for treating pain associated with lumbosacral radiculopathy (LSR) has started.

LSR is a common neuropathic pain condition caused by compression of the nerve roots in the lumbar region of the spine. Common features include pain radiating from the lower back down the legs, together with sensory and motor impairment in the lower limbs. LSR is a very high unmet medical need, affecting 3-5% of the global population and there are no drug treatments currently approved for treating this type of neuropathic pain.

The Phase II trial is a randomised, double-blind, placebo-controlled study designed to evaluate the efficacy and safety of orally administered CNV1014802 in patients with pain associated with LSR. It is an innovative study, incorporating a number of design features which will enhance confidence in the outcome of the study. The trial will run in four European countries and results are expected in the second half of 2012.

Clive Dix, Chief Executive Officer of Convergence Pharmaceuticals, added: "We are delighted to announce the start of this trial; the second clinical stage trial initiated since our conception as a Company in October 2011 and a testament to our innovative team. It is clear that safe, effective pain treatment is urgently required and we are focussed on driving forward the development of our pipeline to meet this need."

Commenting on the announcement, Simon Tate, Chief Scientific Officer of Convergence Pharmaceuticals, said: "We are very excited to be initiating this Phase II study for CNV1014802.  CNV1014802's differentiated and superior profile could have a significant impact on the treatment of patients with pain associated with lumbosacral radiculopathy (LSR), who currently have no approved treatment available to them.  CNV1014802 offers the potential of a safe, effective treatment for this common neuropathic pain."

CNV1014802is a novel small molecule, state-dependent sodium channel blocker that exhibits potency against the Nav1.7 sodium channel. It was recently validated as a key pain target by human genetic linkage. Exciting new data generated by Convergence scientists showed that while displaying a highly state-dependent block of those sodium channels conveying painful sensations, CNV1014802 has a superior and differentiated profile of activity at Nav1.7. This profile translates into significant block of Nav1.7 channels in experimental paradigms which mimic the higher frequency and spontaneous neuronal firing, observed in entrapment neuropathies such as LSR.

CNV1014802 has completed extensive Phase I studies with single and repeated doses in over 150 healthy volunteers, demonstrating an excellent pharmacokinetic and safety profile. CNV1014802 also demonstrated an ideal pharmacokinetic profile together with excellent toleration at doses within the expected therapeutic range.

The need for new drug treatments for chronic pain

The Pain therapeutic area encompasses any disease where pain is a major symptom. The unmet medical need for patients in pain is enormous, with the greatest need being for a more effective therapy that is well tolerated and safe over a long period of time. Within the pain marketplace, current pain treatments are unsatisfactory; overall efficacy is poor (typically 1-2 point reductions on a 10 point scale) and satisfactory to less than 50% of patients. Whilst treatments, such as opioids and non-steroidal anti-inflammatory drugs, are available on the market, many patients obtain little or no relief from these existing analgesics. Often such drugs are associated with adverse events, side effects and addiction concerns, leading to the observation in a recent report by the US Institute of Medicine that a "cultural transformation" is necessary to better prevent, assess, treat, and understand pain of all types.

This highlights the importance of Convergence Pharmaceuticals' goals to develop novel, efficacious analgesics with improved pharmacology and safety profiles.