生物活性

• 描述Lasmiditan is an orally available serotonin (5-HT)1F receptor agonist. Lasmiditan significantly improved the proportions of patients achieving freedom from headache pain and freedom from the most bothersome symptom (photophobia, phonophobia or nausea), relative to placebo, when used to treat a migraine with moderate to severe pain. Lasmiditan is not for use in the preventive treatment of migraine^[3]. 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^[4]. Lasmiditan dosed at 200 and 100 mg was efficacious and well tolerated in the treatment of acute migraine among patients with a high level of cardiovascular risk factors^[5]. Lasmiditan was more effective than placebo for the acute treatment of migraine in patients concurrently using migraine preventive medications. Lasmiditan efficacy and safety measures were similar for patients using and not using preventive medications^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00384774	Migraine	Phase 2	Completed	-	Finland ... more >> Helsinki, Finland Germany Essen, Germany Netherlands Leiden, Netherlands Collapse <<
  NCT00883051	Migraine Disorders	Phase 2	Completed	-	Belgium ... more >> Montegnee, Liege, Belgium, 4420 Hasselt, Limburg, Belgium, 3500 Leuven, Vlaams-Brabant, Belgium, 3000 Brugge, West-Vlaanderen, Belgium, 8000 Bruxelles, Belgium, 1070 Liege, Belgium, 4000 Finland Helsinki, Etelä-Suomi, Finland, 00029 HUS Hyvinkää, Etelä-Suomi, Finland, 05850 Mikkeli, Itä-Suomen Lääni, Finland, 50100 Pori, Länsi-Suomen, Finland, 28100 Jyväskylä, Länsi-Suomi, Finland, 40100 Tampere, Länsi-Suomi, Finland, 33200 Turku, Länsi-Suomi, Finland, 20100 France Nice, Alpes-Maritimes, France, 06002 Bordeaux, Gironde, France, 33076 Toulouse, Haute-Garonne, France, 31059 Lille, Nord, France, 59 037 Rouen, Seine-Maritime, France, 76031 Paris, France, 75010 Germany Freiburg/Breisgau, Baden-Württemberg, Germany, 79106 Göppingen, Baden-Württemberg, Germany, 73033 München, Bayern, Germany, 80802 München, Bayern, Germany, 81377 Wiesbaden, Hessen, Germany, 65189 Erkelenz, Nordrhein-Westfalen, Germany, 41812 Essen, Nordrhein-Westfalen, Germany, 45122 Münster, Nordrhein-Westfalen, Germany, 48129 Itzehoe, Schleswig-Holstein, Germany, 25524 Berlin, Germany, 10117 Bremen, Germany, 28329 Hamburg, Germany, 20246 Spain Sevilla, Andalucía, Spain, 41013 Barcelona, Catalunya, Spain, 08036 Gandia, Comunidad Valenciana, Spain, 46701 Valencia, Comunidad Valenciana, Spain, 46021 Santiago de Compostela, Comunidade Autónoma De Galicia, Spain, 15706 Alcorcon, Madrid, Spain, 28922 Pamplona, Nafarroako Foru Komunitatea, Spain, 31008 Oviedo, Principado De Asturias, Spain, 33007 Collapse <<
  NCT02605174	Migraine With or Without Aura	Phase 3	Completed	-	-

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• 参考文献

• [1] Tfelt-Hansen PC, Olesen J. The 5-HT1F receptor agonist lasmiditan as a potential treatment of migraine attacks: a review of two placebo-controlled phase II trials. J Headache Pain. 2012 Jun;13(4):271-5.

  [2] Nelson DL, Phebus LA, et al. Preclinical pharmacological profile of the selective 5-HT1F receptor agonist lasmiditan. Cephalalgia. 2010 Oct;30(10):1159-69.

  [3] Lamb YN. Lasmiditan: First Approval. Drugs. 2019;79(18):1989-1996

  [4] Capi M, de Andrés F, Lionetto L, et al. Lasmiditan for the treatment of migraine. Expert Opin Investig Drugs. 2017;26(2):227-234

  [5] Kuca B, Silberstein SD, Wietecha L, et al. Lasmiditan is an effective acute treatment for migraine: A phase 3 randomized study. Neurology. 2018;91(24):e2222-e2232

  [6] Loo LS, Ailani J, Schim J, et al. Efficacy and safety of lasmiditan in patients using concomitant migraine preventive medications: findings from SAMURAI and SPARTAN, two randomized phase 3 trials. J Headache Pain. 2019;20(1):84. Published 2019 Jul 24

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