An experimental drug developed in the Faculty of Medicine of the University of Duke could offer a powerful pain relief without the dangerous side effects of opioids.
The medicine, called SBI-810, is part of a new generation of compounds designed to aim at a nerve receiver and spinal cord. While opioids flood multiple cell paths indiscriminately, SBI-810, a non-opioid treatment, adopts a more focused approach, activating only a specific path of pain relief that avoids the euphoric “high” linked to addiction.
In the tests in mice, SBI-810 worked well on its own and, when used in combination, made opioids more effective at lower doses, according to the study published on May 19 in Cell.
“What makes this compound exciting is that it is both analgesic and non-opioid,” said Senior Ru-Rong Ji study author, PHD, an anesthesiology and neurobiology researcher who directs the Duke Anesthesiology Center for Trans Trans Translation Medicine.
Even more encouraging: he avoided common side effects such as constipation and accumulation of tolerance, which often forces patients to need stronger and more frequent doses of opioid over time.
SBI-810 is in early development, but Duke researchers soon sign up for essays in humans and have blocked multiple patents for discovery.
There is an urgent need for pain relief alternatives. Drug overdose deaths are decreasing, but more than 80,000 Americans still die more frequently from opioids every year. Meanwhile, chronic pain affects a third of the American population.
The researchers said that the medicine could be a safer option to treat pain in the short term and chronic for those who recover from surgery or live with diabetic nervous pain.
SBI-810 is designed to go to the neurotensin receiver of the brain receptor 1. Using a method known as biased agonism, it changes a specific signal, β-arrestin-2, linked to pain relief, while avoiding other signals that can cause side effects or addictions.
“The receiver is expressed in sensory neurons and in the brain and spinal cord,” Ji said. “It is a promising objective to treat acute and chronic pain.”
SBI-810 effectively alleviated the pain of surgical incisions, bone fractures and nerve lesions better than some existing analgesics. When injected into mice, it reduced signs of spontaneous discomfort, such as protection and facial grimace.
Duke’s scientists compared SBI-810 with oliceridine, a newer type of opioid used in hospitals, and found that SBI-810 worked better in some situations, with less signs of anguish.
Unlike opioids such as morphine, SBI-810 did not cause tolerance after repeated use. He also beat Gabapentina, a common drug for nervous pain, and did not cause sedation or memory problems, which are often observed with gabapentina.
The researchers said that the double action of the compound, both in peripheral and central nerve systems, could offer a new type of balance in pain medicine: powerful enough to work, but specific enough to avoid damage.
The study was supported by the NIH and the Department of Defense.
The additional authors of Duke include the first authors Ran Guo and Ouyang Chen; Sangsu Bang, Sharat Chandra, Yize Li, Gang Chen, Rou-Gang Xie, Wei He, Jing Xu, Richard Zhou, Shayong Song, Ivan Spasojevic, Marc G. Caron, William C. Wetsel and Lawrence S. Barak. ??