radotinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| tyrosine kinase inhibitors | 5188 | 926037-48-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A second-generation tyrosine kinase inhibitor of Bcr-Abl fusion protein and the platelet-derived growth factor receptor (PDGFR), with potential antineoplastic activity. Upon administration, radotinib specifically inhibits the Bcr-Abl fusion protein, an abnormal enzyme expressed in Philadelphia chromosome-positive chronic myeloid leukemia (CML) cells. In addition, this agent also inhibits PDGFR thereby blocking PDGFR-mediated signal transduction pathways. The inhibitory effect of radotinib on these specific tyrosine kinases may decrease cellular proliferation and inhibit angiogenesis. This agent has shown potent efficacy in CML cells that are resistant to the first-generation standard tyrosine kinase inhibitors, such as imatinib, nilotinib and dasatinib.
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Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 5, 2012 | Korean Food and Drug Administration (KFDA) | IL-Yang |
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:
None
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Chronic myeloid leukemia | indication | 92818009 | DOID:8552 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 11.89 | acidic |
| pKa2 | 6.03 | Basic |
| pKa3 | 4.14 | Basic |
| pKa4 | 3.22 | Basic |
| pKa5 | 1.14 | Basic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Tyrosine-protein kinase ABL1 | Kinase | INHIBITOR | IC50 | 7.51 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| I284LJY110 | UNII |
| 926037-85-6 | SECONDARY_CAS_RN |
| C3273827 | UMLSCUI |
| CHEMBL4297524 | ChEMBL_ID |
| 16063245 | PUBCHEM_CID |
| DB12323 | DRUGBANK_ID |
| 9242 | INN_ID |
| 7814 | IUPHAR_LIGAND_ID |
| C000606751 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
None