Lasmiditan

Lasmiditan

Lasmiditan
Systematic (IUPAC) name
2,4,6-Trifluoro-N-[6-[(1-methyl-4-piperidinyl)carbonyl]-2-pyridinyl]benzamide
Clinical data
Legal status
  • Investigational
Routes Oral, intravenous
Identifiers
ATC code None
PubChem
ChemSpider  N
UNII  YesY
Chemical data
Formula C19H18F3N3O2 
Mol. mass 377.36 g/mol
 N   

Lasmiditan (codenamed COL-144) is an investigational drug for the treatment of acute migraine. It was discovered by Eli Lilly and Company and is being developed by CoLucid Pharmaceuticals. Phase II clinical trial for dose finding purposes were completed in 2007 for an intravenous[1] and in early 2010 for an oral application form.[2]

Mechanism of action

Lasmiditan is a serotonin receptor agonist that, like the unsuccessful LY-334,370, selectively binds to the 5-HT1F receptor subtype. A number of triptans have been shown to act on this subtype as well, but only after their affinity for 5-HT1B and 5-HT1D has been made responsible for their anti-migraine activity. The lack of affinity for these receptors might result in fewer side-effects related to vasoconstriction compared to triptans.[3] A 1998 review has found such side-effects to rarely occur in patients taking triptans,[4] but they are contraindicated for patients with ischaemic heart disease, Raynaud's phenomenon or after a myocardial infarction.[5]

References

  1. ^ ClinicalTrials.gov NCT00384774 A Placebo-Controlled Adaptive Treatment Assignment Study of Intravenous COL-144 in the Acute Treatment of Migraine
  2. ^ ClinicalTrials.gov NCT00883051 Dose-ranging Study of Oral COL-144 in Acute Migraine Treatment
  3. ^ "Molecule of the Month July 2010: Lasmiditan hydrochloride".  
  4. ^ Dahlöf, CG; Mathew, N (1998). "Cardiovascular safety of 5HT1B/1D agonists--is there a cause for concern?". Cephalalgia : an international journal of headache 18 (8): 539–45.  
  5. ^ Mutschler, Ernst; Geisslinger, Gerd; Kroemer, Heyo K.; Schäfer-Korting, Monika (2001). Arzneimittelwirkungen (in German) (8th ed.). Stuttgart: Wissenschaftliche Verlagsgesellschaft. p. 265.