Zatosetron, a 5-HT3 receptor antagonist in a multicenter trial for acute migraine.

Zatosetron (13 mg or 0.19 mg/kg), a potent and selective 5-HT3 receptor antagonist was studied with a 30 min infusion in a crossover double-blind placebo-controlled trial for acute migraine therapy. Groups receiving zatosetron and placebo were demographically similar and zatosetron was well-tolerated in all patients with no clinically significant adverse effects. Migraine severity was reduced in both the placebo and zatosetron groups with no statistically significant differences between zatosetron and placebo. Likewise, no statistically significant differences between placebo and zatosetron treatment groups were identified with regard to migraine duration, overall migraine severity or the relief medication required. Although several limitations of this study exist, these data documenting a lack of benefit of intravenously-administered zatosetron in alleviating the acute pain of migraine add to the list of 5-HT3 receptor antagonists that have failed to support efficacy of this therapeutic modality in the acute treatment of migraine.