Abstract
Gepirone HCL extended-release (gepirone ER; EXXUA™), an oral, selective serotonin (5HT)1A receptor agonist formulated for once-daily administration, has been developed by Fabre-Kramer Pharmaceuticals, Inc. for the treatment of psychiatric disorders, including major depressive disorder (MDD). In September 2023, gepirone ER was approved in the USA for the treatment of adults with MDD. This article summarizes the milestones in the development of gepirone ER leading to this first approval for the treatment of adults with MDD.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
Smith ALW, Harmer CJ, Cowen PJ, et al. The serotonin 1A (5-HT(1A)) receptor as a pharmacological target in depression. CNS Drugs. 2023;37(7):571–85.
Bielski RJ, Cunningham L, Horrigan JP, et al. Gepirone extended-release in the treatment of adult outpatients with major depressive disorder: a double-blind, randomized, placebo-controlled, parallel-group study. J Clin Psychiatry. 2008;69(4):571–7.
World Health Organisation. Depressive disorder (depression). 2023. https://www.who.int/. Accessed 25 Oct 2023.
American Psychological Association. APA clinical practice guideline for the treatment of depression across three age cohorts. 2019. https://www.apa.org/. Accessed 25 Oct 2023.
Feiger AD, Heiser JF, Shrivastava RK, et al. Gepirone extended-release: new evidence for efficacy in the treatment of major depressive disorder. J Clin Psychiatry. 2003;64(3):243–9.
Malhi GS, Bell E, Boyce P, et al. The 2020 Royal Australian and New Zealand College of psychiatrists clinical practice guidelines for mood disorders: Bipolar disorder summary. Bipolar Disord. 2020;22(8):805–21.
Fabre-Kramer Pharmaceuticals Inc. Gepirone ER: US prescribing information 2023. https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm. Accessed 3 Oct 2023.
Fabre-Kramer Pharmaceuticals Inc. Fabre-Kramer Pharmaceuticals announces FDA approval of EXXUA™, the first and only oral selective 5HT1a receptor agonist for the treatment of major depressive disorder in adults [media release]. 28 Sep 2023. https://fabrekramer.com/.
GlaxoSmithKline, Fabre-Kramer Pharmaceuticals Inc. GlaxoSmithKline and Fabre-Kramer Pharmaceuticals enter global agreement for new treatment of major depressive disorder [media release]. 8 Feb 2007. http://www.fabrekramer.com.
PharmaTimes. FDA issues non-approvable letter for GlaxoSmithKline Fabre-Kramer's gepirone ER [media release]. 5 Nov 2007. https://www.pharmatimes.com/.
Fabre-Kramer Pharmaceuticals Inc. Fabre-Kramer looks forward to FDA's decision on gepirone ER for the treatment of major depressive disorder [media release]. 2 Dec 2015. http://www.fabrekramer.com/.
Fabre-Kramer Pharmaceuticals Inc. Fabre-Kramer re-acquires gepirone ER rights from Organon [media release]. 15 Jun 2005. http://www.prnewswire.com.
Chojnacka-Wójcik E, Tatarczyńska E, Gołembiowska K, et al. Involvement of 5-HT1A receptors in the antidepressant-like activity of gepirone in the forced swimming test in rats. Neuropharmacology. 1991;30(7):711–7.
Timmer CJ, Sitsen JMA. Single- and multiple-dose pharmacokinetics and tolerability of gepirone extended-release. Clin Drug Investig. 2002;22(12):819–26.
Fabre LF, Timmer CJ. Effects of food on the bioavailability of gepirone from extended-release tablets in humans: results of two open-label crossover studies. Curr Ther Res Clin Exp. 2003;64(8):580–98.
Dogterom P, Huisman J, Gellert R, et al. Pharmacokinetics of gepirone in subjects with normal renal function and in patients with chronic renal dysfunction. Clin Drug Invest. 2002;22(8):513–22.
Lam YWF, Ereshefsky L, Port A, et al. Effects of rifampin on the disposition of gepirone ER and its metabolites. Open Drug Metabolism Journal. 2009;3:1–7.
Keller MB, Ruwe FJ, Janssens CJ, et al. Relapse prevention with gepirone ER in outpatients with major depression. J Clin Psychopharmacol. 2005;25(1):79–84.
Fabre LF, Brown CS, Smith LC, et al. Gepirone-ER treatment of hypoactive sexual desire disorder (HSDD) associated with depression in women. J Sex Med. 2011;8(5):1411–9.
Fabre LF, Clayton AH, Smith LC, et al. The effect of gepirone-ER in the treatment of sexual dysfunction in depressed men. J Sex Med. 2012;9(3):821–9.
Author information
Authors and Affiliations
Corresponding author
Ethics declarations
Funding
The preparation of this review was not supported by any external funding.
Authorship and Conflict of Interest
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. Susan J. Keam is a contracted employee of Adis International Ltd/Springer Nature, and declares no relevant conflicts of interest. All authors contributed to this article and are responsible for its content.
Ethics Approval, Consent to Participate, Consent to Publish, Availability of Data and Material, Code Availability
Not applicable.
Additional information
This profile has been extracted and modified from the AdisInsight database. AdisInsight tracks drug development worldwide through the entire development process, from discovery, through pre-clinical and clinical studies to market launch and beyond.
Supplementary Information
Below is the link to the electronic supplementary material.
Rights and permissions
Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law.
About this article
Cite this article
Keam, S.J. Gepirone Extended-Release: First Approval. Drugs 83, 1723–1728 (2023). https://doi.org/10.1007/s40265-023-01975-5
Published:
Issue Date:
DOI: https://doi.org/10.1007/s40265-023-01975-5