Convergence commences CNV2197944 multiple ascending dose Phase I study for chronic pain

Phase I Single Dose Study Data Demonstrate Ideal Pharmacokinetic Profile and Excellent Safety and Tolerability

Convergence Pharmaceuticals Limited ("Convergence"), the company focused on the development of novel and high value analgesic medicines, today announces that the multiple ascending dose Phase I study of the novel, first in class calcium channel blocker CNV2197944, for the treatment of chronic pain has been initiated.

The trial is a randomised, placebo controlled Phase I study to investigate the pharmacokinetics, safety and tolerability of orally administered multiple dose regimens of CNV2197944 in both young and elderly volunteers. CNV2197944 is proposed for development initially as a treatment for neuropathic pain and pain associated with osteoarthritis. The study is expected to conclude in 2Q 2012.

The first human single ascending dose Phase I study with orally administered CNV2197944 was recently completed. CNV2197944 was shown to be well absorbed, with an ideal pharmacokinetic profile for the target indication of chronic pain. The compound was well tolerated, with an excellent safety profile.

Clive Dix, Chief Executive Officer of Convergence Pharmaceuticals, commented: "We are really excited to be advancing on schedule to a multiple ascending dose study with this novel, first-in-class treatment for chronic pain.  The data we have seen so far gives us great confidence that CNV2197944 will be a safe and effective long term treatment for chronic pain."

CNV2197944 - a first in class molecule with potential to be a first in class treatment

CNV2197944 is a novel, small molecule, state-dependent calcium channel blocker, designed to selectively inhibit highly active Cav2.2 channels. Preclinical studies demonstrated that CNV2197944 could have analgesic potential for a broad range of chronic pain conditions. Extensive safety and toxicology studies to support the clinical development of CNV2197944 have also been completed, which suggest an excellent margin of safety and tolerability.

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.