SAGE 217

Description: Zuranolone (formerly known as SAGE-217) is a novel and potent GABAA receptor modulator/agonist at both synaptic and extrasynaptic receptor subtypes with EC50s of 296 and 163 nM for alpha1beta2gamma2 and alpha4beta3delta GABAA receptors, respectively, and with excellent oral DMPK properties. SAGE-217 has completed a phase 1 single ascending dose (SAD) and multiple ascending dose (MAD) clinical trial and is currently being studied in parallel phase 2 clinical trials for the treatment of postpartum depression (PPD), major depressive disorder (MDD), and essential tremor (ET). Certain classes of neuroactive steroids (NASs) are positive allosteric modulators (PAM) of synaptic and extrasynaptic GABAA receptors.

References: J Med Chem. 2017 Sep 28; 60(18):7810-7819.