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Brexanolone Injection [Zulresso]

Donald Jeffrey Newport · FDA-approved active Small molecule

Brexanolone is a synthetic neuroactive steroid that acts as a positive allosteric modulator of GABA-A receptors to enhance inhibitory neurotransmission in the brain.

Brexanolone is a synthetic neuroactive steroid that acts as a positive allosteric modulator of GABA-A receptors to enhance inhibitory neurotransmission in the brain. Used for Postpartum depression in adult women.

At a glance

Generic nameBrexanolone Injection [Zulresso]
Also known asZulresso
SponsorDonald Jeffrey Newport
Drug classNeuroactive steroid; GABA-A receptor positive allosteric modulator
TargetGABA-A receptor
ModalitySmall molecule
Therapeutic areaPsychiatry / Neurology
PhaseFDA-approved

Mechanism of action

Brexanolone is the synthetic form of allopregnanolone, an endogenous neurosteroid metabolite of progesterone. It binds to and potentiates GABA-A receptors, increasing chloride channel conductance and neuronal hyperpolarization, thereby enhancing GABAergic inhibitory signaling. This mechanism is thought to restore neurochemical balance in postpartum depression, where allopregnanolone levels are dysregulated.

Approved indications

Common side effects

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