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Jun 23, 2014
 |  BioCentury  |  Product Development

Nav(1.7)igating pain

Convergence data show safety, efficacy of Nav1.7 blocker in neuralgia pain

Data reported by Convergence Pharmaceuticals Ltd. last week for CNV1014802 to treat trigeminal neuralgia gave the first Phase II evidence that systemic Nav1.7 blockers can treat pain safely and effectively. The data also lend further support to the theory that part-time blockage of the channel is enough to be effective.

The Nav1.7 (SCN9A) channel is found on pain-responsive neurons. It was identified as a target for pain disorders in 2006 with the discovery of loss-of-function mutations in members of several families with congenital insensitivity to pain.

Since then several companies have explored the channel as a target for hard-to-treat chronic pain disorders, including rare conditions associated with Nav1.7 gain-of-function mutations, such as erythromelalgia.

The first efficacy data for the class came in 2011 from Xenon Pharmaceuticals Inc.'s TV-45070, a small molecule Nav1.7 blocker.

In a Phase IIa trial in patients with post-herpetic neuralgia (PHN), topical TV-45070 significantly reduced pain scores vs. placebo. Teva Pharmaceutical Industries Ltd. has exclusive worldwide rights to oral and topical formulations of TV-45070.

According to spokesperson Denise Bradley, Teva is studying topical TV-45070 in Phase II to treat osteoarthritis-related pain, and is also investigating its potential in certain neuropathic pain states, such as PHN.

Convergence's study was the first to show both efficacy and safety in a Phase II trial of a systemically delivered Nav1.7 blocker.

It did so in patients with trigeminal neuralgia, a rare condition characterized by paroxysms of severe facial pain that typically last up to two minutes and occur multiple times a day over a course of weeks or months. Pain may be spontaneous or triggered by even light sensations such as touch, chewing or smiling, which leads many patients with poor symptom control to social withdrawal and suicidal ideation.

Traditional analgesics such as opioids don't effectively treat trigeminal neuralgia. Epilepsy drugs such as carbamazepine, a small molecule anticonvulsant, are generally effective. However, they may become less so over time and are often poorly tolerated because of side effects such as drowsiness,...

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