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.
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References
Frieder A, Fersh M, Hainline R, et al. Pharmacotherapy of postpartum depression: current approaches and novel drug development. CNS Drugs. 2019;33(3):265–82.
Kose S, Cetin M. Brexanolone: an allosteric modulator of GABA-A receptors in the rapid treatment of postpartum depression. Psychiatry Clin Psychopharmacol. 2017;27(4):326–8.
Muzik M, Marcus SM, Heringhausen JE, et al. When depression complicates childbearing: guidelines for screening and treatment during antenatal and postpartum obstetric care. Obstet Gynecol Clin N Am. 2009;36(4):771–88.
Schiller CE, Schmidt PJ, Rubinow DR. Allopregnanolone as a mediator of affective switching in reproductive mood disorders. Psychopharmacology. 2014;231:3557–67.
Schiller CE, Meltzer-Brody S, Rubinow D. The role of reproductive hormones in postpartum depression. CNS Spectr. 2015;20(1):48–59.
US FDA. FDA approves first treatment for post-partum depression. 2019. http://www.fda.gov/. Accessed 22 Mar 2019.
Sage Therapeutics Inc. ZULRESSO (Brexanolone): US prescribing information. 2019. http://www.fda.gov/. Accessed 22 Mar 2019.
Zorumski CF, Paul SM, Izumi Y, et al. Neurosteroids, stress and depression: potential therapeutic targets. Neurosci Biobehav Rev. 2013;37(1):109–22.
Hoffmann E, Wald J, Colquhoun H. Evaluation of breast milk concentrations following brexanolone iv administration to healthy lactating women [abstract no. 850]. Am J Obstet Gynecol. 2019;220(1 Suppl):S554.
Kanes S, Colquhoun H, Gunduz-Bruce H, et al. Brexanolone (SAGE-547 injection) in post-partum depression: a randomised controlled trial. Lancet. 2017;390(10093):480–9.
Meltzer-Brody S, Colquhoun H, Riesenberg R, et al. Brexanolone injection in post-partum depression: two multicentre, double-blind, randomised, placebo-controlled, phase 3 trials. Lancet. 2018;392(10152):1058–70.
Kanes SJ, Colquhoun H, Doherty J, et al. Open-label, proof-of-concept study of brexanolone in the treatment of severe postpartum depression. Hum Psychopharmacol. 2017;32(2):e2576.
Clemson C, Meltzer-Brody S, Colquhoun H, et al. Brexanolone iv efficacy in postpartum depression in three pivotal trials: montgomery-asberg depression rating scale assessment [abstract no. 86]. Am J Obstet Gynecol. 2019;220(1 Suppl):S69–70.
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The preparation of this review was not supported by any external funding.
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During the peer review process the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes resulting from any comments received were made by the authors on the basis of scientific completeness and accuracy. Lesley Scott is a salaried employee of Adis/Springer, is responsible for the article content and declares no relevant conflicts of interest.
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Scott, L.J. Brexanolone: First Global Approval. Drugs 79, 779–783 (2019). https://doi.org/10.1007/s40265-019-01121-0
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DOI: https://doi.org/10.1007/s40265-019-01121-0