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4991W93
- Development stage
- Discontinued
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
4991W93 is a **small molecule drug** developed by GSK as a partial agonist at the **5-HT1B** and **5-HT1D** serotonin receptors, with additional activity at **5-HT1A** and **5-HT1F** receptors. It is a conformationally restricted analogue of zolmitriptan, designed to inhibit neurogenic dural plasma protein extravasation without vasoconstriction, and investigated primarily as an antimigraine agent. The drug acts by modulating serotonergic neurotransmission in the trigeminocervical complex, which is implicated in the pathophysiology of migraine. Development was discontinued after reaching phase 2 clinical trials for migraine disorders.
- Other names
- 4-[3-(trans-3-Dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one
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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