Drug intelligence / Profile preview

zolmitriptan

Development stage
Approved
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

Zolmitriptan is a small molecule pharmaceutical drug used for the acute treatment of migraine headaches in adults, with or without aura. It is not indicated for the prevention of migraines or for cluster headaches[1][2][4]. Zolmitriptan belongs to the triptan class and acts as a selective serotonin (5-HT) receptor agonist, primarily targeting 5-HT1B and 5-HT1D receptors, with additional affinity for 5-HT1F[4][5][6]. Its mechanism involves vasoconstriction of intracranial blood vessels and inhibition of pro-inflammatory neuropeptide release from trigeminal nerve endings, thereby reducing migraine pain and associated symptoms such as nausea, photophobia, and phonophobia[2][4][6]. Developed as a second-generation triptan to improve upon earlier agents like sumatriptan, zolmitriptan crosses the blood-brain barrier to exert both central and peripheral effects on migraine pathophysiology[4][6].

Brand names
ZomigZomig-ZMT
Other names
4-((3-(2-(dimethylamino)ethyl)-1H-indol-5-yl)methyl)-2-oxazolidinone(S)-4-((3-(2-(dimethylamino)ethyl)-1H-indol-5-yl)methyl)-2-oxazolidinoneChembl1185Chembl-1185Chembl 1185Zolmitriptan [USAN]ZolmitriptaneZolmitriptanum
02

Targets

HTR1B (5-Hydroxytryptamine Receptor 1B)HTR1D (5-hydroxytryptamine receptor 1D)HTR1F (Serotonin 5-HT1F receptor)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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