Eletriptan is a second-generation 5-hydroxytryptamine(1B/1D) receptor agonist, or triptan, indicated for the acute treatment of migraine. Eletriptan has a favorable pharmacokinetic and pharmacodynamic profile expressed by bioavailability, half-life and high selectivity for cranial arteries. It has been shown to be effective and well tolerated in a wide preapproval development program, which included over 11,000 patients and treated more than 74,000 migraine attacks. In clinical trials, eletriptan has been demonstrated to be one of the most effective oral therapies for the acute treatment of migraine and has shown a very high safety and tolerability profile across the studies performed. Eletriptan showed the most favorable cost-effectiveness profile when compared with other agents in its class.