Engineered Neurotensin Fragments Targeting Neuropathic Pain

DESCRIPTION (provided by applicant): Neuropathic pain management is a major unmet clinical need. Classically used medications, including opioids and non-opioids (primarily NSAIDs), have major side effects associated with their use, and many individuals donot respond to any medications. Neuropathic pain drugs with novel mechanisms of action are being sought as an alternative; however, the only successful FDA-approved drugs, which target calcium channels, have serious limitations to their widespread use. Neurotensin (NT) and its fully active fragment NT(8- 13) have been shown to possess dramatic activity against neuropathic pain when dosed centrally; however, activity is not seen with systemic administration. Halimed Pharmaceuticals has engineered NT(8-13) derivatives that exhibit potent analgesic activity when dosed IV (and, at high concentrations, orally). The compounds are NT-receptor agonists, a novel mechanism of analgesia, thus they may not have the limitations of currently approved medications. We