stiripentol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2480 | 49763-96-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
In animal models, stiripentol antagonizes seizures induced by electric shock, pentetrazole and bicuculline. In rodent models, stiripentol appears to increase brain levels of gamma-aminobutyric acid (GABA) - the major inhibitory neurotransmitter in mammalian brain. This could occur by inhibition of synaptosomal uptake of GABA and/or inhibition of GABA transaminase. Stiripentol has also been shown to enhance GABAA receptor-mediated transmission in the immature rat hippocampus and increase the mean open-duration (but not the frequency) of GABAA receptor chloride channels by a barbiturate-like mechanism. Stiripentol potentiates the efficacy of other anticonvulsants, such as carbamazepine, sodium valproate, phenytoin, phenobarbital and many benzodiazepines, as the result of pharmacokinetic interactions. The second effect of stiripentol is mainly based on metabolic inhibition of several isoenzymes, in particular CYP450 3A4 and 2C19, involved in the hepatic metabolism of other anti-epileptic medicines.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 213.40 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| S (Water solubility) | 13 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 4, 2007 | EMA | BIOCODEX | |
| Aug. 20, 2018 | FDA | BIOCODEX SA |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Status epilepticus | 119.42 | 71.00 | 26 | 392 | 15207 | 63473397 |
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Somnolence | 86.66 | 76.99 | 42 | 666 | 238939 | 79504741 |
| Decreased appetite | 77.84 | 76.99 | 44 | 664 | 342374 | 79401306 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N03AX17 | NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Other antiepileptics |
| MeSH PA | D000927 | Anticonvulsants |
| MeSH PA | D002491 | Central Nervous System Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Myoclonic seizure | indication | 37356005 | |
| Severe myoclonic epilepsy in infancy | indication | 230437002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 250MG | DIACOMIT | BIOCODEX SA | N206709 | Aug. 20, 2018 | RX | CAPSULE | ORAL | Aug. 20, 2023 | NEW CHEMICAL ENTITY |
| 500MG | DIACOMIT | BIOCODEX SA | N206709 | Aug. 20, 2018 | RX | CAPSULE | ORAL | Aug. 20, 2023 | NEW CHEMICAL ENTITY |
| 250MG/PACKET | DIACOMIT | BIOCODEX SA | N207223 | Aug. 20, 2018 | RX | FOR SUSPENSION | ORAL | Aug. 20, 2023 | NEW CHEMICAL ENTITY |
| 500MG/PACKET | DIACOMIT | BIOCODEX SA | N207223 | Aug. 20, 2018 | RX | FOR SUSPENSION | ORAL | Aug. 20, 2023 | NEW CHEMICAL ENTITY |
| 250MG | DIACOMIT | BIOCODEX SA | N206709 | Aug. 20, 2018 | RX | CAPSULE | ORAL | July 14, 2025 | REVISIONS TO THE LABELING TO PROVIDE FOR THE EXPANSION OF THE USE OF STIRIPENTOL FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME IN PATIENTS TAKING CLOBAZAM TO INCLUDE PEDIATRIC PATIENTS WHO ARE 6 MONTHS TO LESS THAN 2 YEARS OF AGE AND WEIGHING 7 KG OR MORE |
| 500MG | DIACOMIT | BIOCODEX SA | N206709 | Aug. 20, 2018 | RX | CAPSULE | ORAL | July 14, 2025 | REVISIONS TO THE LABELING TO PROVIDE FOR THE EXPANSION OF THE USE OF STIRIPENTOL FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME IN PATIENTS TAKING CLOBAZAM TO INCLUDE PEDIATRIC PATIENTS WHO ARE 6 MONTHS TO LESS THAN 2 YEARS OF AGE AND WEIGHING 7 KG OR MORE |
| 250MG/PACKET | DIACOMIT | BIOCODEX SA | N207223 | Aug. 20, 2018 | RX | FOR SUSPENSION | ORAL | July 14, 2025 | NEW PATIENT POPULATION |
| 500MG/PACKET | DIACOMIT | BIOCODEX SA | N207223 | Aug. 20, 2018 | RX | FOR SUSPENSION | ORAL | July 14, 2025 | NEW PATIENT POPULATION |
| 250MG | DIACOMIT | BIOCODEX SA | N206709 | Aug. 20, 2018 | RX | CAPSULE | ORAL | Aug. 20, 2025 | INDICATED FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME (DS) IN PATIENTS 2 YEARS OF AGE AND OLDER TAKING CLOBAZAM |
| 500MG | DIACOMIT | BIOCODEX SA | N206709 | Aug. 20, 2018 | RX | CAPSULE | ORAL | Aug. 20, 2025 | INDICATED FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME (DS) IN PATIENTS 2 YEARS OF AGE AND OLDER TAKING CLOBAZAM |
| 250MG/PACKET | DIACOMIT | BIOCODEX SA | N207223 | Aug. 20, 2018 | RX | FOR SUSPENSION | ORAL | Aug. 20, 2025 | INDICATED FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME (DS) IN PATIENTS 2 YEARS OF AGE AND OLDER TAKING CLOBAZAM |
| 500MG/PACKET | DIACOMIT | BIOCODEX SA | N207223 | Aug. 20, 2018 | RX | FOR SUSPENSION | ORAL | Aug. 20, 2025 | INDICATED FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME (DS) IN PATIENTS 2 YEARS OF AGE AND OLDER TAKING CLOBAZAM |
| 250MG | DIACOMIT | BIOCODEX SA | N206709 | Aug. 20, 2018 | RX | CAPSULE | ORAL | July 14, 2029 | TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME (DS) IN PATIENTS TAKING CLOBAZAM WHO ARE 6 MONTHS TO LESS THAN 2 YEARS OF AGE AND WEIGHING 7 KG OR MORE |
| 500MG | DIACOMIT | BIOCODEX SA | N206709 | Aug. 20, 2018 | RX | CAPSULE | ORAL | July 14, 2029 | TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME (DS) IN PATIENTS TAKING CLOBAZAM WHO ARE 6 MONTHS TO LESS THAN 2 YEARS OF AGE AND WEIGHING 7 KG OR MORE |
| 250MG/PACKET | DIACOMIT | BIOCODEX SA | N207223 | Aug. 20, 2018 | RX | FOR SUSPENSION | ORAL | July 14, 2029 | TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME (DS) IN PATIENTS TAKING CLOBAZAM WHO ARE 6 MONTHS TO LESS THAN 2 YEARS OF AGE AND WEIGHING 7 KG OR MORE |
| 500MG/PACKET | DIACOMIT | BIOCODEX SA | N207223 | Aug. 20, 2018 | RX | FOR SUSPENSION | ORAL | July 14, 2029 | TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME (DS) IN PATIENTS TAKING CLOBAZAM WHO ARE 6 MONTHS TO LESS THAN 2 YEARS OF AGE AND WEIGHING 7 KG OR MORE |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Cytochrome P450 3A4 | Enzyme | WOMBAT-PK | |||||||
| Sodium- and chloride-dependent GABA transporter 1 | Transporter | IC50 | 4.30 | WOMBAT-PK | |||||
| Cytochrome P450 1A2 | Enzyme | WOMBAT-PK | |||||||
| Cytochrome P450 2C19 | Enzyme | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| D05928 | KEGG_DRUG |
| 4038316 | VANDF |
| C0075262 | UMLSCUI |
| CHEBI:94435 | CHEBI |
| CHEMBL1983350 | ChEMBL_ID |
| DB09118 | DRUGBANK_ID |
| 5311454 | PUBCHEM_CID |
| C021092 | MESH_SUPPLEMENTAL_RECORD_UI |
| 5469 | IUPHAR_LIGAND_ID |
| 3760 | INN_ID |
| R02XOT8V8I | UNII |
| 2054968 | RXNORM |
| 132894 | MMSL |
| 23339 | MMSL |
| d06643 | MMSL |
| 012569 | NDDF |
| 427946009 | SNOMEDCT_US |
| 428221002 | SNOMEDCT_US |
| 137767-55-6 | SECONDARY_CAS_RN |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Diacomit | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68418-7939 | CAPSULE | 250 mg | ORAL | NDA | 30 sections |
| Diacomit | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68418-7939 | CAPSULE | 250 mg | ORAL | NDA | 30 sections |
| Diacomit | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68418-7940 | CAPSULE | 500 mg | ORAL | NDA | 30 sections |
| Diacomit | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68418-7940 | CAPSULE | 500 mg | ORAL | NDA | 30 sections |
| Diacomit | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68418-7941 | POWDER, FOR SUSPENSION | 250 mg | ORAL | NDA | 30 sections |
| Diacomit | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68418-7941 | POWDER, FOR SUSPENSION | 250 mg | ORAL | NDA | 30 sections |
| Diacomit | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68418-7942 | POWDER, FOR SUSPENSION | 500 mg | ORAL | NDA | 30 sections |
| Diacomit | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68418-7942 | POWDER, FOR SUSPENSION | 500 mg | ORAL | NDA | 30 sections |