Zolmitriptan, a selective 5-HT(1B/D) agonist was developed for the acute treatment of migraine. Dose-finding studies show a clearly defined dose response curve for the oral formulation with onset of efficacy demonstrated within 45 min of dosing. Clinical trials support its efficacy in all types of migraine, with excellent safety and tolerability in those patients for whom zolmitriptan is not contraindicated. Future developments, including new formulations, will provide patients with a greater choice of treatment.