MEDI 255 |
| Neuropathic pain is a chronic pain state, where the nerve-fibers are damaged or injured. This leads to misfiring of the neurons and eventually to a change in the function of the nerve in the injured area. Neuropathic pain or neuralgia can have multiple causes, and is most often suffered by patients with diabetes (diabetic neuropathy), HIV (HIV-related neuropathic pain), and herpes (post-herpetic neuralgia). Patients who have neuropathic pain describe it as a burning sensation or an electric shock, and have compared it to sitting on needles and pins. The most commonly used drugs are anti-epileptic agents, anti-depressants, local anesthetics, and narcotics. Unfortunately, the current therapies are efficacious in only a fraction of the patient population and leave physicians with limited treatment options. Most molecules in use to date are active against multiple targets. With the exception of the narcotics, their most common denominator is activity on sodium or calcium channels. We believe that a rational, channel specific approach will lead to better therapeutics for this area of drug discovery. Therefore, we have developed a comprehensive platform that combines high throughput screening for ion channels, medicinal chemistry, and in vivo neuropathic pain pharmacology. This offers us the opportunity to rapidly identify and develop new profiles with molecules specifically designed for the treatment of neuropathic pain, and potentially for other nervous system diseases where ion channels play a critical role. In this presentation, we will discuss our screening technology (E-VIPR), which allowed us to evaluate our corporate collection as well as known drugs for their sodium and calcium channel activity. We will show data for molecules that compare favorably with known drugs. We will also discuss animal models for neuropathic pain and the effect of subtype specific NaV blockers in these models. |
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Hot Topics in Medicinal Chemistry
1:30 PM-4:00 PM, Wednesday, August 22, 2007 BCEC -- 210 B/C, Oral
Division of Medicinal Chemistry |