Neuropathic pain is a hyperalgesic pain condition resulting from dysfunction of the peripheral or central nervous system. Neuropathic pain is associated with a variety of etiologies, including trauma, infection, diabetes, immune deficiencies, ischemic disorders, and toxic neuropathies. It is estimated that 1.4 million people per year in the US are diagnosed with diabetic neuropathy, trigeminal neuralgia, or post-herpetic neuralgia. Other causes include multiple sclerosis, post-stroke pain, HIV-associated pain, herpes virus infection, and cancer. Approximately 26 million patients are affected worldwide and the lifestyle of these patients can be severely impeded, a problem compounded by the lack of efficacy and frequent incidence of side effects associated with current treatment options. Opioids are frequently ineffective in treating neuropathic pain. Current treatments, such as gabapentin (Neurontin TM ), involve non-selective regulation of neurotransmitter systems or ion channels and generally result in significant dose-limiting CNS side effects. In this area where no current single drug treatment is effective in more than 50% of patients, novel therapeutic approaches are an urgent priority. The world market for neuropathic pain management is projected to reach approximately $1.5 billion by 2010.