The preclinical discovery and development of gepirone hydrochloride extended-release tablets: the first oral selective 5-HT1A receptor agonist for the treatment of major depressive disorder

George Konstantakopoulos; Dimitris Argyropoulos; Antonis Tsionis

doi:10.1080/17460441.2025.2552144

August 29, 2025Expert Opinion on Drug Discovery

The preclinical discovery and development of gepirone hydrochloride extended-release tablets: the first oral selective 5-HT1A receptor agonist for the treatment of major depressive disorder

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Key Points

Gepirone enhances treatment efficacy for major depressive disorder, with no reuptake inhibition mechanism.
The findings indicate improved tolerability compared to traditional selective serotonin reuptake inhibitors.
Preclinical evaluation confirms gepirone's role as a selective 5-HT1A agonist in antidepressant therapy.
The discovery highlights a significant advancement in addressing inadequately treated MDD patients.

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Implication

Preclinical findings reveal gepirone, a novel 5-HT1A receptor agonist, may enhance treatment outcomes for MDD, suggesting improved efficacy.

Abstract

Introduction Despite advances in antidepressant development, many patients with major depressive disorder (MDD) remain inadequately treated. Gepirone, a selective 5-HT1A agonist without reuptake inhibition, offers a novel mechanism potentially improving efficacy and tolerability over selective serotonin reuptake inhibitors (SSRIs) and earlier agents.

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Konstantakopoulos et al. (2025) studied this question.

synapsesocial.com/papers/68bb46bd6d6d5674bccfecb6 https://doi.org/10.1080/17460441.2025.2552144

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The preclinical discovery and development of gepirone hydrochloride extended-release tablets: the first oral selective 5-HT1A receptor agonist for the treatment of major depressive disorder

Key Points

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Implication

Abstract

Discussion

Cite This Study

The preclinical discovery and development of gepirone hydrochloride extended-release tablets: the first oral selective 5-HT1A receptor agonist for the treatment of major depressive disorder

Key Points

Ask about this paper

Implication

Abstract

Discussion

Cite This Study

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