gavestinel

Gavestinel is a highly potent and selective non-competitive antagonist at the strychnine-insensitive glycine binding site of the N-methyl-D-aspartate (NMDA) receptor-channel complex. It was developed as a neuroprotective agent for acute ischemic stroke and acts by inhibiting NMDA receptor activation via the glycine co-agonist site rather than the glutamate site. This mechanism was intended to reduce excitotoxic neuronal damage during ischemic events such as stroke. Gavestinel demonstrated high affinity (Kd = 0.8 nM) and selectivity (>1000-fold over NMDA, AMPA, and kainate sites), with oral bioavailability and in vivo activity in preclinical models. Despite promising preclinical results showing reduced infarct volume without significant side effects common to other NMDA antagonists (such as cognitive or cardiovascular effects), two large phase III clinical trials failed to show efficacy in improving outcomes after acute ischemic stroke[1][2][3][4][5][7].

Other names

gavestinel