&NA;Lubeluzole (R 87926, JK 8792, Prosynap®), a benzothiazole derivative, is a neuroprotectant under development with Janssen (Johnson and Johnson) for the treatment of acute ischaemic stroke. Its neuroprotective effects are favoured to be mediated via the prevention of nitric oxide-induced neuronal cell death. Janssen has initiated the regulatory approval process for lubeluzole in the USA and Europe. However, the case made for approval hinges on a meta-analysis of functional outcome in 2 independent phase III trials, whereby, to resolve a significant level of efficacy, it was necessary to exclude patients over 75 years of age with severe stroke.Phase III trials are also being conducted in Europe, Canada and Australia. Janssen-Kyowa (a joint venture between Janssen and Kyowa Hakko) is also developing lubeluzole in Japan, where it is currently undergoing phase I clinical trials.Lubeluzole is a novel benzothiazole compound that may exert its neuroprotective effects by inhibition of the glutamate-activated nitric oxide synthase pathway. High doses of lubeluzole have been associated with adverse cardiovascular events and safety concerns. However, lower doses of lubeluzole have been associated with modest clinical improvement and no major toxicity issues. Lubeluzole has had a favourable effect on mortality in patients with mild to moderate ischaemic stroke, but does not appear to be beneficial in severe stroke. Large studies to further define the role of lubeluzole in acute ischaemic stroke are underway.