Brexanolone: First Global Approval

@article{Scott2019BrexanoloneFG,
  title={Brexanolone: First Global Approval},
  author={Lesley J. Scott},
  journal={Drugs},
  year={2019},
  volume={79},
  pages={779-783}
}
  • L. Scott
  • Published 1 May 2019
  • Biology, Medicine
  • Drugs
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… 

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References

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Open‐label, proof‐of‐concept study of brexanolone in the treatment of severe postpartum depression

TLDR
Brexanolone (USAN; formerly SAGE‐547 Injection), a proprietary injectable allopregnanolone formulation, was evaluated as a treatment for severe PPD in a proof‐of‐concept, open‐label study.

Brexanolone: an allosteric modulator of GABA-A receptors in the rapid treatment of postpartum depression

TLDR
Findings lend support to the hypothesis that changes in neuroactive steroid concentrations during pregnancy and postpartum are capable of provoking affective dysregulation in mothers and reflect the relative involvement of various functional neuroanatomical systems.

Pharmacotherapy of Postpartum Depression: Current Approaches and Novel Drug Development

TLDR
A recent series of open-label and placebo-controlled randomized clinical trials of brexanolone in postpartum depression demonstrated a rapid reduction in depressive symptoms, and has led to the submission for regulatory approval to the US Food and Drug Administration.

Allopregnanolone as a mediator of affective switching in reproductive mood disorders

TLDR
The role of the “neuroactive” steroids estradiol and progesterone in reproductive endocrine-related mood disorders are described and potential mechanisms by which ALLO might contribute to their pathophysiology are highlighted.

The role of reproductive hormones in postpartum depression

TLDR
The hypothesis that fluctuations in reproductive hormone levels during pregnancy and the postpartum period trigger PPD in susceptible women is examined to propose that these women constitute a “hormone-sensitive” PPD phenotype, which should be studied independent of other PPD phenotypes to identify underlying pathophysiology and develop novel treatment targets.