Alliance of DAMGO and NK1 Derived Pharmacophores in Discovering Potent µ-Preferring Multivalent Ligands for the Treatment of Pain

Technology #ua15-051

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Researchers
Victor Hruby
Regents Professor Emeritus, Chemistry & Biochemistry
Aswini Giri
Assistant Research Scientist, Chemistry & Biochemistry
Managed By
Paul Eynott
Sr. Licensing Manager (520) 621-2878

Technology ID: UA15-051

Technology Background: People around the world suffer from various forms of unwanted pain. Unfortunately, there is no drug that can effectively counteract pain states, especially sustained and neuropathic pain. Opioids are a class of pain medications that are widely used to treat acute, severe, and cancer pain. However, regular use of opioid drugs is accompanied by serious undesirable effects, including drowsiness, mental clouding, nausea, emesis, and constipation. In addition, opioid drugs are highly abused, and consistent opioid therapy leads to the development of analgesic tolerance and increased sensitivity to pain in many patients. There is evidence that sustained pain can cause neuroplastic modification in both ascending and descending pathways in the spinal column, which leads to augmented release of neurotransmitters that intensify pain and increase expression of the corresponding receptors responsible for promoting pain. Therefore, there is a great need for novel design strategies in the development of next-generation pain medications to provide pain relief without the undesirable side effects seen with current medications.

Invention: This technology consists of novel multivalent ligands that feature a combination of μ-δ opioid agonists and NK1 antagonists for the treatment of pain.

Advantages: One advantage of the current invention is that the mixture of the μ-δ opioid agonists and NK1 antagonists has synergistic effects in the management of prolonged pain that provide potent analgesic effects in acute and neuropathic pain. The technology offers increased blood brain barrier permeability without the unwanted side of opioid-induced tolerance and reward liability. By combining the μ-δ opioid agonists and NK1 antagonists into a single ligand, the technology has better metabolic and pharmacological properties compared to co-administering separate drugs targeting these individual pathways. Finally, the multivalent ligands provide higher concentrations of bioavailability compared to co-administration of separate drugs because the expression of the NK1 and opioid receptions as well as the neurotransmitters shows a significant degree of overlap in the central nervous system.

Applications: This technology offers rationally designed, multi-targeted compounds as novel therapeutics for the treatment of patients suffering from acute and chronic pain. More specifically, the invention provides novel μ-δ opioid agonists and NK1 antagonists compounds for acute and chronic pain relief, and for acute and chronic intervention for drug abuse. The technology may be applied as a stand-along pain management therapy, or as an adjunctive therapy alongside other pain management medications and/or techniques.

Patent Status: Provisional Patent Pending

Lead Inventor: Dr. Victor Hruby

Licensing Manager: Paul Eyenot