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gepirone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| anxiolytics, buspirone derivatives | 4562 | 83928-76-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Gepirone is indicated for the treatment of major depressive disorder in adults. The mechanism of its antidepressant effect is not fully understood but is thought to be related to its modulation of serotonergic activity in the CNS through selective agonist activity at 5HT1A receptors.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 15 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,MAP3K21,MAP3K7,MAPK7,NTRK2,PDK2,PIK3CB,PRKDC,SIK2,SIK3,STK33,TEK | 27 | |||
| kinase-selectivity-class | AXL,BRAF,CDK9,STK33,TEK | 5 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 0.451 | Moderate | 0.74 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 0 | Moderate | 0.74 | |
| rat-kpuu-brain | Rat brain Kpuu | 0.231 | % | Moderate | 0.74 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 22, 2023 | FDA | FABRE-KRAMER PHARMACEUTICALS, INC. |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N06AX19 | NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Other antidepressants |
| MeSH PA | D000928 | Antidepressive Agents |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D014149 | Tranquilizing Agents |
| MeSH PA | D014151 | Anti-Anxiety Agents |
| MeSH PA | D017366 | Serotonin Receptor Agonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018490 | Serotonin Agents |
| CHEBI has role | CHEBI:35469 | antidepressant |
| CHEBI has role | CHEBI:35474 | anxiolytic drug |
| CHEBI has role | CHEBI:35941 | serotonergic agonist |
Related Drugs by ATC class:
N06AX Other antidepressants 28 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Major depressive disorder | indication | 370143000 | |
| Severe hepatic impairment | contraindication | 59927004 | |
| Prolonged QT interval | contraindication | 111975006 | |
| Congenital long QT syndrome | contraindication | 442917000 | |
| Monoamine oxidase inhibitor | contraindication | 734595009 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.51 | Basic |
| pKa2 | 2.23 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 18.2MG BASE | EXXUA | FABRE KRAMER | N021164 | Sept. 22, 2023 | RX | TABLET, EXTENDED RELEASE | ORAL | 7538116 | Sept. 2, 2030 | TREATMENT OF SUBJECTS WITH MAJOR DEPRESSION WITH SEXUAL DYSFUNCTION CAUSED BY EITHER MAJOR DEPRESSION OR PRIOR TREATMENTS, OR TREATMENT OF SUBJECTS WITH MAJOR DEPRESSION WITHOUT THE RISK OF SEXUAL DYSFUNCTION ADVERSE REACTIONS |
| EQ 36.3MG BASE | EXXUA | FABRE KRAMER | N021164 | Sept. 22, 2023 | RX | TABLET, EXTENDED RELEASE | ORAL | 7538116 | Sept. 2, 2030 | TREATMENT OF SUBJECTS WITH MAJOR DEPRESSION WITH SEXUAL DYSFUNCTION CAUSED BY EITHER MAJOR DEPRESSION OR PRIOR TREATMENTS, OR TREATMENT OF SUBJECTS WITH MAJOR DEPRESSION WITHOUT THE RISK OF SEXUAL DYSFUNCTION ADVERSE REACTIONS |
| EQ 54.5MG BASE | EXXUA | FABRE KRAMER | N021164 | Sept. 22, 2023 | RX | TABLET, EXTENDED RELEASE | ORAL | 7538116 | Sept. 2, 2030 | TREATMENT OF SUBJECTS WITH MAJOR DEPRESSION WITH SEXUAL DYSFUNCTION CAUSED BY EITHER MAJOR DEPRESSION OR PRIOR TREATMENTS, OR TREATMENT OF SUBJECTS WITH MAJOR DEPRESSION WITHOUT THE RISK OF SEXUAL DYSFUNCTION ADVERSE REACTIONS |
| EQ 72.6MG BASE | EXXUA | FABRE KRAMER | N021164 | Sept. 22, 2023 | RX | TABLET, EXTENDED RELEASE | ORAL | 7538116 | Sept. 2, 2030 | TREATMENT OF SUBJECTS WITH MAJOR DEPRESSION WITH SEXUAL DYSFUNCTION CAUSED BY EITHER MAJOR DEPRESSION OR PRIOR TREATMENTS, OR TREATMENT OF SUBJECTS WITH MAJOR DEPRESSION WITHOUT THE RISK OF SEXUAL DYSFUNCTION ADVERSE REACTIONS |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 18.2MG BASE | EXXUA | FABRE KRAMER | N021164 | Sept. 22, 2023 | RX | TABLET, EXTENDED RELEASE | ORAL | Sept. 22, 2028 | NEW CHEMICAL ENTITY |
| EQ 36.3MG BASE | EXXUA | FABRE KRAMER | N021164 | Sept. 22, 2023 | RX | TABLET, EXTENDED RELEASE | ORAL | Sept. 22, 2028 | NEW CHEMICAL ENTITY |
| EQ 54.5MG BASE | EXXUA | FABRE KRAMER | N021164 | Sept. 22, 2023 | RX | TABLET, EXTENDED RELEASE | ORAL | Sept. 22, 2028 | NEW CHEMICAL ENTITY |
| EQ 72.6MG BASE | EXXUA | FABRE KRAMER | N021164 | Sept. 22, 2023 | RX | TABLET, EXTENDED RELEASE | ORAL | Sept. 22, 2028 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| D(2) dopamine receptor | GPCR | Ki | 7.24 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | AGONIST | Ki | 7.89 | CHEMBL | ||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 5.44 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 7.50 | CHEMBL | |||||
| Serotonin 1 (5-HT1) receptor | GPCR | IC50 | 6.17 | CHEMBL | |||||
| Adrenergic receptor alpha-1 | GPCR | Ki | 5.62 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4044261 | VANDF |
| CHEBI:135990 | CHEBI |
| CHEMBL284092 | ChEMBL_ID |
| C039979 | MESH_SUPPLEMENTAL_RECORD_UI |
| 12930 | IUPHAR_LIGAND_ID |
| 5676 | INN_ID |
| DB12184 | DRUGBANK_ID |
| JW5Y7B8Z18 | UNII |
| 2672253 | RXNORM |
| 371477 | MMSL |
| 41993 | MMSL |
| d10111 | MMSL |
| 019595 | NDDF |
| 019596 | NDDF |
| C0066624 | UMLSCUI |
| A1ESA | PDB_CHEM_ID |
| CHEMBL1204187 | ChEMBL_ID |
| 55191 | PUBCHEM_CID |
| 83928-66-9 | SECONDARY_CAS_RN |
| JW5Y7B8Z18 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| EXXUA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 23594-150 | TABLET, EXTENDED RELEASE | 18.20 mg | ORAL | NDA | 29 sections |
| EXXUA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 23594-151 | TABLET, EXTENDED RELEASE | 36.30 mg | ORAL | NDA | 29 sections |
| EXXUA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 23594-152 | TABLET, EXTENDED RELEASE | 54.50 mg | ORAL | NDA | 29 sections |
| EXXUA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 23594-153 | TABLET, EXTENDED RELEASE | 72.60 mg | ORAL | NDA | 29 sections |