NeurOp’s technology to optimize selective and context-dependent NMDA inhibitors has led to the discovery of several proprietary compounds. Screening for drug-like properties among this group of compounds led to the identification of NP10679.

shutterstock_115530445Properties of NP10679

  • NP10679 is selective for a specific NMDA subtype, GluN2B, and has increased potency in acidic conditions.
    • Over 100-fold more potent at GluN2B-containing NMDA receptors than other subtypes
    • 6-fold greater potency in lower pH (acidic) environments, a context relevant to a number of CNS disorders
  • Excellent drug-like properties, such as brain penetrance, half-life, oral bioavailability and weak CYP inhibition.
  • Effective in animal models of stroke, subarachnoid hemorrhage (SAH), perioperative pain (preliminary data) and opiate relapse (preliminary data)
  • Phase 1 clinical studies indicate excellent pharmacokinetics in humans
  • Phase 1 studies also suggest good safety margins for a number of possible indications such as stroke, SAH and acute severe pain

After successful preclinical development, NP10679 is currently in Phase 1 clinical trials.