title: Lasmiditan for the treatment of migraine.
abstract: Migraine is one of the most common diseases in the world, with high economical and subjective burden. Migraine acute therapy is nowadays based on specific and non-specific drugs but up to 40% of episodic migraineurs still have unmet treatment needs and over 35% do not benefit from triptans administration. Serotonin-1F receptors have been identified in trigeminal system and became an ideal target for anti-migraine drug development as potential trigeminal neural inhibitors. Lasmiditan, a novel serotonin1F receptor agonist, showed specific affinity in vitro for the receptor without any vasoconstrictive action and inhibited markers associated with electrical stimulation of trigeminal ganglion in migraine animal models. Areas covered: This article reviews both preclinical and clinical studies on lasmiditan as a potential acute therapy for migraine, as well as pharmacokinetic and pharmacodynamic features. It also summarizes safety and tolerability data gathered in the various human studies. Expert opinion: The absence of vasoconstrictive effects makes lasmiditan a promising novel migraine acute therapy. Although preclinical and Phase I and II studies established a significant efficacy, the limited knowledge about pharmacokinetics and metabolism, the high rate of non-serious central nervous system side effects and the lack of larger studies remain still a matter of concern that should be addressed in future studies.
authors.affiliation: a Experimental Immunology Laboratory , Fondazione Luigi Maria Monti, IDI-IRCCS , Rome , Italy.
authors.forename: Matilde
authors.initials: M
authors.lastname: Capi
authors.affiliation: b CICAB Clinical Research Centre , Extremadura University Hospital and Medical School , Badajoz , Spain.|c Department of Analytical Chemistry and Food Technology, Faculty of Pharmacy , University of Castilla-La Mancha , Albacete , Spain.
authors.forename: Fernando
authors.initials: F
authors.lastname: de Andrés
authors.affiliation: d Advanced Molecular Diagnostic Unit , Fondazione Luigi Maria Monti, IDI-IRCCS , Rome , Italy.
authors.forename: Luana
authors.initials: L
authors.lastname: Lionetto
authors.affiliation: e NESMOS Department , Sapienza University of Rome , Rome , Italy.
authors.forename: Giovanna
authors.initials: G
authors.lastname: Gentile
authors.affiliation: e NESMOS Department , Sapienza University of Rome , Rome , Italy.
authors.forename: Fabiola
authors.initials: F
authors.lastname: Cipolla
authors.affiliation: f Department of Clinical and Molecular Medicine , Sapienza University , Rome , Italy.|g Regional Referral Headache Centre , Sant'Andrea Hospital , Rome , Italy.
authors.forename: Andrea
authors.initials: A
authors.lastname: Negro
authors.affiliation: e NESMOS Department , Sapienza University of Rome , Rome , Italy.
authors.forename: Marina
authors.initials: M
authors.lastname: Borro
authors.affiliation: f Department of Clinical and Molecular Medicine , Sapienza University , Rome , Italy.|g Regional Referral Headache Centre , Sant'Andrea Hospital , Rome , Italy.
authors.forename: Paolo
authors.initials: P
authors.lastname: Martelletti
authors.affiliation: f Department of Clinical and Molecular Medicine , Sapienza University , Rome , Italy.|g Regional Referral Headache Centre , Sant'Andrea Hospital , Rome , Italy.|h Department of Neurology and Psychiatry , Sapienza University of Rome , Rome , Italy.|i Bipolar & Psychotic Disorders Program , McLean Hospital , Belmont , MA , USA.
authors.forename: Martina
authors.initials: M
authors.lastname: Curto
mesh_terms: D000818:Animals; D001549:Benzamides / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D004195:Disease Models, Animal; D015195:Drug Design; D006801:Humans; D008881:Migraine Disorders / Q000188:drug therapy* / Q000503:physiopathology; D010880:Piperidines / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D011725:Pyridines / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism; D017366:Serotonin Receptor Agonists / Q000009:adverse effects / Q000627:therapeutic use*; D000096642:Receptor, Serotonin, 5-HT1F
chemical_list: D001549:Benzamides; D010880:Piperidines; D011725:Pyridines; D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists; D000096642:Receptor, Serotonin, 5-HT1F; C554777:lasmiditan
keywords: 5-HT1F receptor; Migraine; acute; clinical trials; lasmiditan