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omaveloxolone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| steroids not used as glucocorticosteroids | 5712 | 1474034-05-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
The precise mechanism by which omaveloxolone exerts its therapeutic effect in patients with Friedreich’s ataxia is unknown. Omaveloxolone have been shown to activate the Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway in vitro and in vivo in animals and humans. The Nrf2 pathway is involved in the cellular response to oxidative stress.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 4.304 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.687 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 51.404 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 20.654 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.400 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 1.360 | % | High | 1 |
| herg | hERG pIC50 | 5.035 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 15.885 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 88.512 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.640 | % | High | 1 |
| kinase-safety-class | ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,MAP3K7,MAPK10,MAPK7,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CD,PLK1,PRKDC,STK33,SYK,TEK | 31 | |||
| kinase-selectivity-class | GRK2,PDK1 | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.321 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 17.298 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.440 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 8.570 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 1 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | Moderate | 0.71 | |
| pppb | Pig plasma protein binding (% unbound) | 0.690 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 31.915 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 6 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.490 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 8.995 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 28, 2023 | FDA | REATA PHARMACEUTICALS INC |
FDA Adverse Event Reporting System (Female)
None
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 |
|---|---|---|---|---|---|---|
| Hepatic cytolysis | 63.71 | 51.26 | 16 | 214 | 55037 | 110534032 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N07XX25 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS OTHER NERVOUS SYSTEM DRUGS Other nervous system drugs |
| FDA MoA | N0000185506 | Cytochrome P450 3A4 Inducers |
| FDA MoA | N0000187063 | Cytochrome P450 2C8 Inducers |
| CHEBI has role | CHEBI:22586 | antioxidant |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:67079 | anti-inflammatory agent |
| CHEBI has role | CHEBI:77307 | cardioprotective agent |
Related Drugs by ATC class:
N07XX Other nervous system drugs 23 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Friedreich’s ataxia | indication | 10394003 | DOID:12705 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 50MG | SKYCLARYS | BIOGEN US | N216718 | Feb. 28, 2023 | RX | CAPSULE | ORAL | 11091430 | April 20, 2029 | TREATMENT OF FRIEDREICHS ATAXIA IN ADULTS AND ADOLESCENTS AGED 16 YEARS AND OLDER |
| 50MG | SKYCLARYS | BIOGEN US | N216718 | Feb. 28, 2023 | RX | CAPSULE | ORAL | 11919838 | April 20, 2029 | METHOD OF TREATING FRIEDRICHS ATAXIA BY ACTIVATING THE NRF2 PATHWAY |
| 50MG | SKYCLARYS | BIOGEN US | N216718 | Feb. 28, 2023 | RX | CAPSULE | ORAL | 11919838 | April 20, 2029 | METHOD OF TREATING FRIEDRICHS ATAXIA BY ACTIVATING THE NRF2 PATHWAY WHICH REDUCES OXIDATIVE STRESS |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 50MG | SKYCLARYS | BIOGEN US | N216718 | Feb. 28, 2023 | RX | CAPSULE | ORAL | Dec. 20, 2027 | INFORMATION ADDED TO CLINICAL PHARMACOLOGY SECTION |
| 50MG | SKYCLARYS | BIOGEN US | N216718 | Feb. 28, 2023 | RX | CAPSULE | ORAL | Feb. 28, 2028 | NEW CHEMICAL ENTITY |
| 50MG | SKYCLARYS | BIOGEN US | N216718 | Feb. 28, 2023 | RX | CAPSULE | ORAL | Feb. 28, 2030 | TREATMENT OF FRIEDREICHS ATAXIA IN ADULTS AND ADOLESCENTS AGED 16 YEARS AND OLDER |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Nuclear factor erythroid 2-related factor 2 | Transcription factor | ACTIVATOR | IC50 | 9.40 | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| CHEBI:229661 | CHEBI |
| CHEMBL4303525 | ChEMBL_ID |
| C000589490 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7573 | IUPHAR_LIGAND_ID |
| DB12513 | DRUGBANK_ID |
| 4042120 | VANDF |
| C4519135 | UMLSCUI |
| 10135 | INN_ID |
| 71811910 | PUBCHEM_CID |
| 365409 | MMSL |
| 41269 | MMSL |
| d10017 | MMSL |
| 019329 | NDDF |
| D10964 | KEGG_DRUG |
| G69Z98951Q | UNII |
| 2631931 | RXNORM |
| G69Z98951Q | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| SKYCLARYS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64406-250 | CAPSULE | 50 mg | ORAL | NDA | 30 sections |
| SKYCLARYS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 73179-250 | CAPSULE | 50 mg | ORAL | NDA | 29 sections |