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oxetorone
- Development stage
- Unknown
- Lead developer
- Labaz
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Oxetorone is a small molecule drug classified as a benzoxepine derivative, primarily used as an antimigraine agent. It acts mainly as a non-selective serotonin receptor antagonist, with additional antihistamine (H1 receptor antagonist) and alpha-blocking properties. Antidopaminergic effects are also suspected due to observed cases of hyperprolactinemia and extrapyramidal symptoms. Its therapeutic effect in migraine prophylaxis is attributed to the combined antagonism of serotonin, histamine, and alpha-adrenergic receptors[2][4][5][9]. The drug has been marketed in several European countries for the disease-modifying treatment of migraines[4]. Adverse effects can include drowsiness, hypertonia, gastrointestinal disturbances (such as diarrhea or lymphocytic colitis), and rare but potentially severe toxicities at high doses[7].
- Brand names
- NocertoneOxedix
- Other names
- oxetoronaoxetorone fumarate
02
Targets
HRH1 (Histamine H1 Receptor)DRD2 (Dopamine D2 Receptor)5-HT2 (5-HT2 receptor family)ADRA1A (α1A)
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