Peripheral Opioid Analgesia

Scientists have shown that opioid receptors are present on nerve endings in the skin, joints, eyes and visceral organs. Activation of these opioid receptors, which are outside of the central nervous system, with opioid analgesics potentially reducing pain related to injury or inflammation by decreasing pain signal transmission from the peripheral nerves into the spinal cord. Proof-of-concept studies in animals and humans have shown that small doses of morphine, applied locally to inflamed tissues such as skin, joints and eyes are effective in reducing pain. These findings have created the opportunity for us to potentially develop an entirely new class of analgesics that may selectively stimulate opioid receptors in inflamed tissues but not stimulate opioid receptors in the central nervous system, thereby avoiding the central nervous system side effects of opioids. These pain medications are called peripheral analgesics. In preclinical studies, our peripheral mu agonists have demonstrated efficacy in models of inflammatory pain. Our peripheral kappa agonists have demonstrated efficacy in preclinical models of visceral and inflammatory pain. Because our peripheral analgesics are designed to have limited ability to cross the blood-brain barrier at therapeutic doses, they have the potential to avoid addiction or other adverse central nervous system side effects, such as sedation or decreased respiratory function or addiction.


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