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2018 ; 15
(2
): 291-303
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Targeted 5-HT(1F) Therapies for Migraine
#MMPMID29488143
Vila-Pueyo M
Neurotherapeutics
2018[Apr]; 15
(2
): 291-303
PMID29488143
show ga
Migraine is a common neurological disease characterised by the presence of
attacks of unilateral, severe head pain accompanied by other symptoms. Although
it has been classified as the sixth most disabling disorder, the available
therapeutic options to treat this condition have not progressed accordingly. The
advance in the development of 5-HT(1) receptor agonists for migraine, including
5-HT(1B/D) and 5-HT(1F) receptor agonists, has meant a major step forward towards
the progression of a better treatment for migraine. Triptans have a limited
efficacy, and their effect on vasoconstriction makes them unsafe for patients
with cardiovascular and/or cerebrovascular diseases. Therefore, novel effective
antimigraine treatments without cardiovascular effects are required, such as
selective 5-HT(1F) receptor agonists (ditans). Lasmiditan has much higher
affinity for the 5-HT(1F) receptor than for the vasoconstrictor 5-HT(1B)
receptor. This has been confirmed in preclinical studies performed to date, where
lasmiditan showed no effect on vasoconstriction, and in clinical trials, where
healthy individuals and patients did not report cardiac events due to treatment
with lasmiditan, although it should be confirmed in larger cohorts. Lasmiditan
crosses the blood-brain barrier and may act both centrally and peripherally on
5-HT(1F) receptors expressed on trigeminal neurons. It is a well-tolerated
compound that does not induce major adverse events. Although ongoing phase III
clinical trials are needed to confirm its efficacy and safety, lasmiditan might
offer an alternative to treat acute migraine with no associated cardiovascular
risk. This review will focus on the characterisation of 5-HT(1) receptor agonists
and their effects as migraine therapies.
|Animals
[MESH]
|Benzamides/pharmacology/*therapeutic use
[MESH]
|Clinical Trials as Topic
[MESH]
|Humans
[MESH]
|Migraine Disorders/*drug therapy
[MESH]
|Piperidines/pharmacology/*therapeutic use
[MESH]
|Pyridines/pharmacology/*therapeutic use
[MESH]
|Receptor, Serotonin, 5-HT1F
[MESH]
|Receptors, Serotonin, 5-HT1/metabolism
[MESH]
|Receptors, Serotonin/*metabolism
[MESH]
|Serotonin 5-HT1 Receptor Agonists/*therapeutic use
[MESH]
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