The neuroprotectant lubeluzole is a benzothiazole compound in late clinical evaluation for the treatment of acute ischaemic stroke. In experimental animals, lubeluzole prevents extracellular glutamate increase following ischaemia, inhibits glutamate-induced nitric oxide-related neurotoxicity and normalises neuronal excitability in the peri-infarct region. Animal models have shown lubeluzole to decrease infarct size following middle cerebral artery occlusion. Promising results in phase I trials of cardiac safety led to a phase II study investigating the effect of lubeluzole, 10 or 20 mg/day, on mortality and neurological and functional recovery in acute ischaemic stroke. Despite an increased mortality rate in the 20 mg/day group, later confirmed as an imbalance of randomisation unrelated to the drug, this trial showed that lubeluzole, 10 mg/day, was well tolerated and reduced mortality. A phase III trial has been recently completed and it is hoped that its results will confirm these findings.