gepirone

Gepirone, sold under the brand name Exxua, is a medication used for the treatment of major depressive disorder. It is taken orally.

Key facts

Drug.O: 2
Drug.tradename: Exxua
Drug.width2: 260
Drug.N: 5
Drug.Watchedfields: changed
Drug.verifiedrevid: 437181944
Drug.image: Gepirone.svg
Drug.image_class: skin-invert-image
Drug.width: 250
Drug.image2: Gepirone_3D_ball-and-stick.png
Drug.routes_of_administration: By mouth
Drug.ATC_prefix: N06
Drug.ATC_suffix: AX19
Drug.legal_US: Rx-only
Drug.bioavailability: 14–17%
Drug.protein_bound: 72%
Drug.metabolism: CYP3A4
Drug.metabolites: 3'-OH-gepirone; 1-(2-Pyrimidinyl)piperazine

via Wikipedia infobox

Chemical data

Formula: C19H29N5O2
Molecular weight: 359.5 g/mol
IUPAC name: 4,4-dimethyl-1-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]piperidine-2,6-dione

via PubChem

Drug data · ChEMBL

Max clinical phase: Approved
Molecule type: Small molecule
First approval: 2023
Admin. routes: oral
Indications: cocaine dependence, major depressive disorder

via ChEMBL · EBI

Research

310 papers

Gepirone.2006
Gepirone Extended-Release: First Approval.Drugs · 2023
Gepirone hydrochloride: a novel antidepressant with 5-HT1A agonistic properties.Drugs of today (Barcelona, Spain : 1998) · 2019
Gepirone: A New Extended-Release Oral Selective Serotonin Receptor Agonist for Major Depressive Disorder.The Journal of pharmacy technology : jPT : official publication of the Association of Pharmacy Technicians · 2024
Gepirone for Major Depressive Disorder: From Pharmacokinetics to Clinical Evidence: A Narrative Review.International journal of molecular sciences · 2025

via PubMed

Wikidata facts

Mass: 359.232

Show 2 more facts

chemical formula: C₁₉H₂₉N₅O₂
canonical SMILES: CC1(CC(=O)N(C(=O)C1)CCCCN2CCN(CC2)C3=NC=CC=N3)C

Sources (3)

via Wikidata · CC0

~7 min read

Article

20 sections

Contents

Medical uses
Available forms
Specific populations
Contraindications
Side effects
Interactions
Pharmacology
Pharmacodynamics
Pharmacokinetics
Absorption
Distribution
Metabolism
Elimination
Chemistry
History
Society and culture
Names
Research
See also
References

Gepirone, sold under the brand name Exxua, is a medication used for the treatment of major depressive disorder. It is taken orally.

Side effects of gepirone include dizziness, nausea, insomnia, abdominal pain, and dyspepsia (indigestion). Gepirone acts as a partial agonist of the serotonin 5-HT1A receptor. An active metabolite of gepirone, 1-(2-pyrimidinyl)piperazine, is an α2-adrenergic receptor antagonist. Gepirone is a member of the azapirone group of compounds.