sepranolone

Sepranolone is a neuroactive steroid and the endogenous isomer of allopregnanolone, developed as a pharmaceutical agent for neurological and psychiatric disorders. It acts as a negative allosteric modulator of the GABA-A receptor, specifically antagonizing the effects of allopregnanolone without affecting GABA itself or other GABA-A agonists. Sepranolone was primarily investigated for premenstrual dysphoric disorder (PMDD), menstrual migraine, and Gilles de la Tourette's syndrome. The drug was originally developed by Asarina Pharma (originator Umecrine Mood) and later acquired by Relmada Therapeutics. Clinical studies have shown that sepranolone can significantly reduce PMDD symptoms when administered during the luteal phase, with additional evidence supporting its efficacy in reducing tics in Tourette's syndrome[1][3][4][5][8]. Its mechanism offers high selectivity with minimal off-target CNS effects[6].

Brand names

Sepranolone

Other names

isoallopregnanolone