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Method patent issued for investigational new class of pain medication
Date:1/25/2013

y of RTX that investigates the safety and efficacy of RTX administered intrathecally to advanced cancer patients with severe pain. The study continues to recruit patients, and more information can be found at:

http://cancerpainstudynih.com and www.clinicaltrials.gov

RTX first came to the attention of researchers in the mid 1970s when German scientists isolated it as the active compound in a dried white resin and centuries-old folk remedy that is extracted from a spiny, cactus-like plant called Euphorbia resinifera. The discovery soon caught the investigative eye of Dr. Peter Blumberg, a scientist with NIH's National Cancer Institute (NCI). He was intrigued by RTX's unique chemical structure, a natural hybrid between capsaicin, the irritant in red peppers, and daphnane, a unique class of plant-derived, irritant compounds.

Blumberg received several patents in the United States and abroad during the late 1980s and early 1990s related to RTX. He and his colleagues showed among their many discoveries that the compound was a 1,000 times more potent than capsaicin when binding to the surface of certain types of heat-pain sensing neurons. While Blumberg and colleagues laid the scientific groundwork, the optimal means to administer RTX as a new, ultra-potent class of pain medication remained open for discovery.

In the early 2000s, Dr. Michael Iadarola, a basic scientist with NIH's National Institute of Dental and Craniofacial Research (NIDCR), and colleagues began to piece together one such alternative. They had homed in on RTX's reported unique ability to bind to a much studied protein called vanilloid receptor 1 (VR1), which is a channel, or pore, displayed on the surface of certain types of heat-pain-sensing neurons, or nerve cells. RTX attaches to VR1, and, like water flowing through a hose, prompts an influx of calcium ions through the channel
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Contact: Bob Kuska
kuskar@nidcr.nih.gov
301-594-7560
NIH/National Institute of Dental and Craniofacial Research
Source:Eurekalert

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