Tezampanel & NGX426 for Migraine & Pain
Tezampanel, an intravenously administered compound, and NGX426, the oral prodrug of tezampanel, are first-in-class compounds that may represent novel treatments for both pain and non-pain indications. Tezampanel and NGX426 are ionotropic glutamate receptor antagonists that target the AMPA and kainate sub-type receptors. While normal glutamate production is essential, excess glutamate production, either through injury or disease, has been implicated in a number of diseases and disorders. Tezampanel and NGX426 are the first glutamate receptor antagonists with this combined binding activity to be tested in humans.
By acting at both the AMPA and kainate receptor site to competitively block the binding of glutamate, both tezampanel and NGX426 have the potential to treat a number of diseases and disorders. These include chronic pain, such as migraine and neuropathic pain, muscle spasticity and a condition known as central sensitization, a persistent state of hypersensitivity to pain that is a core component of many pain conditions.
Development Status
Results of a Phase 2b clinical trial of tezampanel were released in October 2007. In the trial, a single dose of tezampanel given by injection was statistically significant compared to placebo in treating acute migraine headache. This was the sixth Phase 2 trial in which tezampanel has been shown to have analgesic activity. Based on a review of the Phase 2 data, the FDA previously agreed that tezampanel may move forward into a Phase 3 program for in acute migraine.
In November 2009, Raptor announced the presentation of clinical trial data on NGX426 at the 12th International Conference on the Mechanisms and Treatment of Neuropathic Pain, held on November 20-21 in San Francisco. The results of the study led by Mark Wallace, M.D., Professor of Clinical Anesthesiology at the Center for Pain Medicine of the University of California at San Diego, suggested that NGX426 could be effective in a variety of neuropathic pain states, which are caused by damage to or dysfunction of the peripheral or central nervous system rather than stimulation of pain receptors.
In February 2009, results from a Phase 1 multiple dose trial of NGX426 showed that the compound is safe and well-tolerated in healthy male and female subjects when dosed once daily for five consecutive days.
Raptor is currently seeking program funding, a development collaboration or an out-licensing partner for the migraine and pain program.
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