tezampanel

Tezampanel is a small molecule drug originally developed by Eli Lilly that acts as a competitive antagonist of the AMPA and kainate subtypes of the ionotropic glutamate receptor family, with selectivity for the GluK5 subtype of the kainate receptor[1][2][3]. It has neuroprotective and anticonvulsant properties, likely due to its ability to block calcium uptake into neurons. Tezampanel has demonstrated analgesic, antihyperalgesic, anxiolytic effects in animal studies and suppresses opioid withdrawal symptoms as well as tolerance development[1][6]. It has been investigated for use in acute migraine therapy (Phase II), pain (acute or chronic), cluster headaches, opiate withdrawal syndrome, neuropathic pain, anxiety disorders, and seizure disorders[2][3][4][5][6]. The drug is currently being developed by Proniras for opiate withdrawal syndrome; previous clinical trials in migraine were discontinued[4][6].

Other names

tezampanel (anhydrous)tezampanel hydrate