Lasmiditan, also known as COL-144 and LY573144, is a novel, centrally acting, highly selective 5-HT(1F) receptor agonist (K1=2.21 μM) without vasoconstrictor activity that seemed effective when given as an intravenous infusion in a proof-of-concept migraine study. Lasmiditan showed efficacy in its primary endpoint, with a 2-hour placebo-subtracted headache response of 28.8%, though with frequent reports of dizziness, paresthesias, and vertigo.
Sheng, Xiaohong; Sheng, Xiaoxia; Jiang, Xiawei. Preparation of crystalline form of lasmiditan and its pharmaceutical composition. Assignee SoliPharma LLC, Peop. Rep. China. WO 2018010345. (2018).
Carniaux, Jean-Francois; Cummins, Jonathan. Compositions and methods of synthesis of pyridinoylpiperidine derivatives as 5-HT1F agonists for treating and preventing migraine. Assignee Colucid Pharmaceuticals, Inc., USA. WO 2011123654. (2011).
Cohen, Michael Philip; Kohlman, Daniel Timothy; Liang, Sidney Xi; Mancuso, Vincent; Victor, Frantz; Xu, Yao-Chang; Ying, Bai-Ping; Zacherl, Deanna Piatt; Zhang, Deyi. Preparation of pyridinoylpiperidines as 5-HT1F agonists. Assignee Eli Lilly and Company, USA. WO 2003084949. (2003).
