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brexanolone

Trade name: Zulresso

Small moleculeapprovedBreakthrough Therapy FDA

Approved

Mar 19, 2019

Allopregnanolone is a neurosteroid metabolite of progesterone. It is an allosteric modulator of inhibitory γ-aminobutyric acid (GABA-A) receptors on neural stem cells and other cell types in the brain. Allopregnanolone has effects similar to those of other positive allosteric modulators of the GABA action at GABAA receptor such as the benzodiazepines, including anxiolytic, sedative, and anticonvulsant activity. A solution of allopregnanolone, SAGE-547 is an intravenous allosteric modulator of both synaptic and extrasynaptic γ-aminobutyric acid type A (GABAA)receptors. It's believed that allopregnanolone is effective as an anticonvulsant when prolonged seizure activity has become resistant to benzodiazepine treatment. Under the names brexanolone and SAGE-547, allopregnanolone is under development by SAGE Therapeutics as an intravenously administered drug for the treatment of super-refractory status epilepticus, postpartum depression, and essential tremor. Allopregnanolone is in phase III trials for the treatment of super-refractory status epilepticus (SRSE) and postpartum depression. — NCATS

Clinical trial activity

33 trials · 26 clinical orgs · 1 marketing orgs

Phase 1
8
Phase 2
20
Phase 3
6
Phase 4
4

Earliest trial started Apr 1, 2013 (NCT01673828)

Timeline

2010s

  1. Jan 1, 2013

    Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2014

    Sage Therapeutics — Earliest Phase 1 Sponsor(trial)

  3. Jan 1, 2015

    Sage Therapeutics — Earliest Phase 3 Sponsor(trial)

  4. Mar 19, 2019

    Sage Therapeutics — Earliest FDA Approval

  5. Mar 19, 2019

    Sage Therapeutics — Marketing Organization

  6. Mar 19, 2019

    Sage Therapeutics — NDA Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewBreakthroughMar 19, 2019

Chemistry & pharmacology

Loading structure…

SMILES

CC(=O)[C@H]1CC[C@H]2[C@@H]3CC[C@H]4C[C@H](O)CC[C@]4(C)[C@H]3CC[C@]12C
Mol. weight
318.5 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Parenteral
Availability
Prescription Only

Oral

No

Parenteral

Yes

Topical

No

Black box warningFirst in class

Sources

Also known as

  • allopregnanolone
  • allopregnanolone
  • allopregnanolone
  • brexanolone
  • sage-547
  • sage-547

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07161700Phase 2Sep 2, 2025Collaborative Neuroscience Research, Premier Research Group, Seaport Therapeutics
NCT07079761Phase 2Aug 4, 2025Harvard University, National Institute of Mental Health (NIMH)
NCT07065240Phase 2Jun 19, 2025Collaborative Neuroscience Research, Premier Research Group, Seaport Therapeutics
NCT06979544Phase 3Jun 16, 2025Lipocine Inc.
NCT06580444Phase 2Oct 24, 2024Department of Defense, Department of Veteran Affairs, Pharmacotherapies for Alcohol and Substance Abuse Consortium, RTI International, Sage Therapeutics, Yale University
NCT06263010Phase 1Jan 12, 2024University of Arizona
NCT05645432Phase 2Mar 31, 2023Sage Therapeutics
NCT05329779Phase 4Nov 4, 2022Harvard University
NCT05223829Phase 1Nov 1, 2022National Institute on Alcohol Abuse and Alcoholism (NIAAA), Sage Therapeutics, Yale University
NCT05254405Phase 4Mar 1, 2022Sage Therapeutics, University of Texas, Austin
NCT05314153Early Phase 1 (Phase 1)Feb 23, 2022Sage Therapeutics, University of North Carolina at Chapel Hill
NCT04468360Phase 2Jan 31, 2022Boston University, National Institute of Mental Health (NIMH)
NCT05129865Phase 1Dec 31, 2021Novotech, PureTech
NCT05059600Phase 4Nov 30, 2021Sage Therapeutics
NCT04838301Phase 2Nov 30, 2021ADM Diagnostics, Inc., National Institute on Aging (NIA), Syneos Health, University of Arizona, University of Southern California
NCT04537806Phase 3Nov 30, 2020Sage Therapeutics
NCT04273191Phase 4Feb 29, 2020Sage Therapeutics
NCT04015869Phase 1Jul 1, 2019Yale University
NCT04003285Phase 2Jul 1, 2019Department of Veteran Affairs
NCT03748303Phase 1May 31, 2019Alzheimer's Association, University of Arizona, University of Southern California
Showing 20 of 33 trials
Page 1 / 2

Organizations

Research & Development (26)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Sage TherapeuticsFor profit181452014
Harvard UniversityAcademic/Hospital4242015
University of ArizonaAcademic/Hospital3222019
University of Southern CaliforniaAcademic/Hospital3222014
Yale UniversityAcademic/Hospital3222019
Collaborative Neuroscience ResearchAcademic/Hospital2012025
Department of DefenseGovernment2012013
Department of Veteran AffairsGovernment2112019
National Institute of Mental Health (NIMH)Government2012022
National Institute on Aging (NIA)Government2022014
Premier Research GroupFor profit2012025
Seaport TherapeuticsFor profit2212025
University of California, DavisAcademic/Hospital2212013
ADM Diagnostics, Inc.For profit1012021
Alzheimer's AssociationAcademic/Hospital1012019
Boston UniversityAcademic/Hospital1112022
Lipocine Inc.For profit1112025
National Institute on Alcohol Abuse and Alcoholism (NIAAA)Government1012022
Northwestern UniversityAcademic/Hospital1012015
NovotechFor profit1012021
26 organizations
Page 1 / 2

Marketing (2)

OrganizationOrg typeRelationshipDate
Sage TherapeuticsFor profitMKTGMar 19, 2019
Sage TherapeuticsFor profitNDAMar 19, 2019