Kainate Receptor Antagonists to Treat Neuropathic Pain

Period of Performance: 05/31/1999 - 05/30/2000


Phase 2 SBIR

Recipient Firm

Annovis, Inc.
Aston, PA 19014
Principal Investigator


ArnaX, a division of Bearsden Bio, Inc., has developed novel compounds that selectively regulate glutamate receptor subtypes for treatment of CNS disorders. In Phase I, we demonstrated that SYM 2081, a potent and selective antagonist of the kainic acid receptor (KAR), can reduce sensitivity to painful stimuli in established animal models of both acute and chronic neuropathic pain at doses that do not impair motor activity. Having established that KAR modulation by SYM 2081 is feasible for treating neuropathic pain in vivo, we are seeking Phase II funding to develop SYM 2081, or another KAR-selective antagonist, as a lead candidate for treatment of this condition. Such a therapeutic agent would fulfill a tremendous unmet need since opiates and ketamine (by continuous i.v. infusion) are the only available compounds that can alleviate neuropathic pain. Additional criteria for a lead candidate are: (a) t1/2>1.8 hours in vivo and (b)no development of tolerance. Having identified a lead candidate, we will initiate the preclinical studies required by the FDA. Data collected during the Phase II project will be invaluable for securing the additional funding and/or a corporate partner for commercializing our novel therapeutic agent for neuropathic pain. PROPOSED COMMERCIAL APPLICATIONS: The goal of this project is to commercialize the novel compounds that selectively modulate activity of the kainate receptor as therapeutic agents for the treatment of pain due to injury, diabetic neuropathy, and other neurological disorders.