Brexanolone: First Global Approval

Drugs. 2019 May;79(7):779-783. doi: 10.1007/s40265-019-01121-0.

Abstract

Brexanolone (ZULRESSO™) is an intravenously administered, small molecule, neuroactive steroid GABAA receptor positive allosteric modulator that was developed by Sage Therapeutics under license to the University of California for the treatment of postpartum depression (PPD). The formulation is a mixture of allopregnanolone, an endogenous inhibitory pregnane neurosteroid, and sulfobutylether-beta-cyclodextrin (a solubilizing agent). In mid-March 2019 brexanolone received its first global approval in the USA for the treatment of PPD in adult women. This article summarizes the milestones in the development of brexanolone leading to its first approval for the treatment of adult women with PPD.

MeSH terms

  • Administration, Intravenous / methods
  • Adolescent
  • Adult
  • Allosteric Regulation / drug effects
  • Depression, Postpartum / drug therapy*
  • Drug Approval
  • Drug Combinations
  • Drug Therapy, Combination / methods
  • Female
  • Humans
  • Male
  • Middle Aged
  • Pregnanolone / administration & dosage
  • Pregnanolone / adverse effects
  • Pregnanolone / pharmacokinetics*
  • Pregnanolone / pharmacology
  • Pregnanolone / therapeutic use
  • Receptors, Steroid / metabolism
  • Treatment Outcome
  • United States
  • United States Food and Drug Administration
  • beta-Cyclodextrins / administration & dosage
  • beta-Cyclodextrins / adverse effects
  • beta-Cyclodextrins / pharmacokinetics*
  • beta-Cyclodextrins / pharmacology
  • beta-Cyclodextrins / therapeutic use

Substances

  • Drug Combinations
  • Receptors, Steroid
  • beta-Cyclodextrins
  • brexanolone
  • SBE4-beta-cyclodextrin
  • Pregnanolone