Drug intelligence / Profile preview

zuranolone

Development stage
Approved
Lead developer
Sage Therapeutics
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Zuranolone is an orally administered neuroactive steroid antidepressant used for the treatment of postpartum depression (PPD) in adults. It acts as a positive allosteric modulator of the gamma-aminobutyric acid type A (GABA-A) receptor, enhancing both synaptic and extrasynaptic GABAergic signaling. This mechanism is distinct from traditional monoamine-based antidepressants and benzodiazepines; zuranolone binds to a non-benzodiazepine site on the GABA-A receptor, allowing it to potentiate both phasic and tonic inhibitory currents. The drug was developed by Sage Therapeutics and Biogen and received FDA approval in August 2023 as the first oral therapy specifically indicated for PPD. Clinical trials have also investigated its use in major depressive disorder (MDD), showing rapid onset of action with significant improvement in depressive symptoms[1][2][3][5][6][8].

Brand names
Zurzuvae
Other names
zuranolone
02

Targets

GABRR (GABA-A receptor subunit rho)

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