Lasmiditan
| Systematic (IUPAC) name | |
|---|---|
| 2,4,6-Trifluoro-N-[6-[(1-methyl-4-piperidinyl)carbonyl]-2-pyridinyl]benzamide | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | Investigational |
| Routes | Oral, intravenous |
| Identifiers | |
| ATC code | None |
| PubChem | CID 11610526 |
| UNII | 760I9WM792 |
| Chemical data | |
| Formula | C19H18F3N3O2 |
| Mol. mass | 377.36 g/mol |
| SMILES | eMolecules & PubChem |
| |
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]
[edit] 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 less 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]
[edit] References
- ^ ClinicalTrials.gov NCT00384774 A Placebo-Controlled Adaptive Treatment Assignment Study of Intravenous COL-144 in the Acute Treatment of Migraine
- ^ ClinicalTrials.gov NCT00883051 Dose-ranging Study of Oral COL-144 in Acute Migraine Treatment
- ^ "Molecule of the Month July 2010: Lasmiditan hydrochloride". Prous Science. http://www.prous.com/molecules/default.asp?ID=198. Retrieved 2011-08-03.
- ^ 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. doi:10.1046/j.1468-2982.1998.1808539.x. PMID 9827245.
- ^ Mutschler, Ernst; Geisslinger, Gerd; Kroemer, Heyo K.; Schäfer-Korting, Monika (2001) (in German). Arzneimittelwirkungen (8th ed.). Stuttgart: Wissenschaftliche Verlagsgesellschaft. p. 265. ISBN 978-3-8047-1763-3. OCLC 47700647.
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