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ataluren 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 4872 | 775304-57-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A nonsense mutation in DNA results in a premature stop codon within an mRNA. This premature stop codon in the mRNA causes disease by terminating translation before a full-length protein is generated. Ataluren enables ribosomal readthrough of mRNA containing such a premature stop codon, resulting in production of a full-length protein.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 2.80 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 60 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.891 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.211 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 107.399 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 8.610 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 1.540 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 2.480 | % | High | 1 |
| herg | hERG pIC50 | 4.277 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 10.209 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.899 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.720 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,ERBB2,FLT3,GRK2,GSK3B,IKBKB,ITK,JAK1,JAK2,MAP2K6,MAP3K21,MAP3K7,MAP4K1,MAPK7,MAPKAPK2,MARK4,MTOR,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1 | 47 | |||
| kinase-selectivity-class | ACVR2B,AXL,BRAF,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,KDR,MAP3K21,MAPK7,PDK4,PRKDC,SIK2,STK33,TTK | 16 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 4.853 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 17.378 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 3.310 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.542 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.400 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 13.092 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 70.150 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.780 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 557.186 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 31, 2014 | EMA | PTC Therapeutics International Limited |
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 | M09AX03 | MUSCULO-SKELETAL SYSTEM OTHER DRUGS FOR DISORDERS OF THE MUSCULO-SKELETAL SYSTEM OTHER DRUGS FOR DISORDERS OF THE MUSCULO-SKELETAL SYSTEM Other drugs for disorders of the musculo-skeletal system |
Related Drugs by ATC class:
M09AX Other drugs for disorders of the musculo-skeletal system 11 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Duchenne muscular dystrophy | indication | 76670001 | DOID:11723 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.43 | acidic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Flavin reductase (NADPH) | Enzyme | Kd | 6.70 | CHEMBL | |||||
| Histone deacetylase 6 | Enzyme | IC50 | 6.52 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| K16AME9I3V | UNII |
| D09323 | KEGG_DRUG |
| C2930764 | UMLSCUI |
| CHEBI:94805 | CHEBI |
| CHEMBL256997 | ChEMBL_ID |
| 11219835 | PUBCHEM_CID |
| DB05016 | DRUGBANK_ID |
| 8956 | INN_ID |
| C515878 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7341 | IUPHAR_LIGAND_ID |
| 015935 | NDDF |
| 1263915001 | SNOMEDCT_US |
| 718843009 | SNOMEDCT_US |
| JBF | PDB_CHEM_ID |
Pharmaceutical products:
None