Lasmiditan
Encyclopedia
Lasmiditan is an investigational drug for the treatment of acute migraine
Migraine
Migraine is a chronic neurological disorder characterized by moderate to severe headaches, and nausea...

. It was discovered by Eli Lilly and Company
Eli Lilly and Company
Eli Lilly and Company is a global pharmaceutical company. Eli Lilly's global headquarters is located in Indianapolis, Indiana, in the United States...

 and is being developed by CoLucid Pharmaceuticals. Phase II clinical trial
Clinical trial
Clinical trials are a set of procedures in medical research and drug development that are conducted to allow safety and efficacy data to be collected for health interventions...

 for dose finding purposes were completed in 2007 for an intravenous and in early 2010 for an oral application form.

Mechanism of action

Lasmiditan is a serotonin receptor agonist
Serotonin receptor agonist
A serotonin receptor agonist is a compound that activates serotonin receptors, mimicking the effect of the neurotransmitter serotonin. There are various serotonin receptors and ligands.-5-HT1A receptor:...

 that, like the unsuccessful LY-334,370, selectively binds to the 5-HT1F receptor subtype. A number of triptan
Triptan
Triptans are a family of tryptamine-based drugs used as abortive medication in the treatment of migraines and cluster headaches. They were first introduced in the 1990s...

s have been shown to act on this subtype as well, but only after their affinity for 5-HT1B
5-HT1B receptor
5-hydroxytryptamine receptor 1B also known as the 5-HT1B receptor is a protein that in humans is encoded by the HTR1B gene. The 5-HT1B receptor is a 5-HT receptor subtype.-Tissue distribution and function:...

 and 5-HT1D
5-HT1D receptor
5-hydroxytryptamine receptor 1D, also known as HTR1D, is a 5-HT receptor, but also denotes the human gene encoding it. 5-HT1D acts on the central nervous system, and affects locomotion and anxiety...

 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
Vasoconstriction
Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels, particularly the large arteries, small arterioles and veins. The process is the opposite of vasodilation, the widening of blood vessels. The process is particularly important in...

 compared to triptans. A 1998 review has found such side-effects to rarely occur in patients taking triptans, but they are contraindicated for patients with ischaemic heart disease
Ischaemic heart disease
Ischaemic or ischemic heart disease , or myocardial ischaemia, is a disease characterized by ischaemia of the heart muscle, usually due to coronary artery disease...

, Raynaud's phenomenon
Raynaud's phenomenon
In medicine, Raynaud's phenomenon is a vasospastic disorder causing discoloration of the fingers, toes, and occasionally other areas. This condition can also cause nails to become brittle with longitudinal ridges. Named for French physician Maurice Raynaud , the phenomenon is believed to be the...

 or after a myocardial infarction
Myocardial infarction
Myocardial infarction or acute myocardial infarction , commonly known as a heart attack, results from the interruption of blood supply to a part of the heart, causing heart cells to die...

.
The source of this article is wikipedia, the free encyclopedia.  The text of this article is licensed under the GFDL.
 
x
OK