Drug intelligence / Profile preview

gepirone

Development stage
Approved
Lead developer
Fabre-Kramer Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Gepirone is an oral antidepressant of the azapirone class, approved for the treatment of major depressive disorder (MDD) in adults. It acts as a selective partial agonist at the serotonin 5-HT1A receptor, modulating serotonergic activity in the central nervous system. Gepirone and its active metabolite 3’-OH-gepirone bind to 5-HT1A receptors as agonists, while another metabolite (1-PP) acts as an antagonist at alpha2-adrenergic receptors. Unlike some other antidepressants, gepirone has minimal affinity for dopamine D2 receptors and is associated with a lower risk of sexual dysfunction. The drug was developed to address limitations of earlier antidepressants and is available in extended-release tablet form[2][4][5][7][8].

Brand names
Exxua
Other names
gepirone hydrochlorideTravivo
02

Targets

HTR2A (Serotonin receptor 5-HT2A)ADRA2A (α2A)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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